Recent publications

2019

Amat-Foraster M, Celada P, Richter U, Jensen AA, Plath N, Artigas F, Herrik KF. Modulation of thalamo-cortical activity by the NMDA receptor antagonists ketamine and phencyclidine in the awake freely-moving rat. Neuropharmacology 158: 107745 (2019).

Foster SR, Hauser AS, Vedel L, Strachan RT, Huang XP, Gavin AC, Shah SD, Nayak AP, Haugaard-Kedström LM, Penn RB, Roth BL, Bräuner-Osborne H*, Gloriam DE*. Discovery of Human Signaling Systems: Pairing Peptides to G Protein-Coupled Receptors. Cell 179: 895-908 (2019). * Shared last authors.

Gaiser BI, Danielsen M, Marcher-Rørsted E, Røpke Jørgensen K, Wróbel TM, Frykman M, Johansson H, Bräuner-Osborne H, Gloriam DE, Mathiesen JM, Sejer Pedersen D. Probing the Existence of a Metastable Binding Site at the β2-Adrenergic Receptor with Homobivalent Bitopic Ligands. J. Med. Chem. 62: 7806-7839 (2019).

Giraudo A, Krall J, Bavo F, Nielsen B, Kongstad KT, Rolando B, De Blasio R, Gloriam DE, Löffler R, Thiesen L, Harpsøe K, Frydenvang K, Boschi D, Wellendorph P, Lolli ML, Jensen AA, Frølund B. Five-Membered N-Heterocyclic Scaffolds as Novel Amino Bioisosteres at γ-Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters. J. Med. Chem. 62: 5797-5809 (2019).

Griem-Krey N, Klein AB, Herth M, Wellendorph P. Autoradiography as a Simple and Powerful Method for Visualization and Characterization of Pharmacological Targets. J. Vis. Exp. 145: e58879 (2019).

Jørgensen, C.V., S.J. Gasparini, J. Tu. H. Zhou, M.J. Seibel and H. Bräuner-Osborne. Metabolic and skeletal homeostasis are maintained in full locus GPRC6A knockout mice. Sci. Rep. 9: 5995 (2019).

Jørgensen, C.V., H. Zhou, M.J. Seibel and H. Bräuner-Osborne. Label-free dynamic mass redistribution analysis of endogenous adrenergic receptor signaling in primary preadipocytes and differentiated adipocytes. J. Pharmacol. Toxicol. Methods 97: 59-66 (2019).

Koehl A, Hu H, Feng D, Sun B, Zhang Y, Robertson MJ, Chu M, Kobilka TS, Laeremans T, Steyaert J, Tarrasch J, Dutta S, Fonseca R, Weis WI, Mathiesen JM, Skiniotis G, Kobilka BK. Structural insights into the activation of metabotropic glutamate receptors. Nature 566: 79-84 (2019).

Krall J, Bavo F, Falk-Petersen CB, Jensen CH, Nielsen JO, Tian Y, Anglani V, Kongstad KT, Piilgaard L, Nielsen B, Gloriam DE, Kehler J, Jensen AA, Harpsøe K, Wellendorph P, Frølund B. Discovery of 2-(Imidazo[1,2- b]pyridazin-2-yl)acetic Acid as a New Class of Ligands Selective for the γ-Hydroxybutyric Acid (GHB) High-Affinity Binding Sites. J. Med. Chem. 62: 2798-2813 (2019).

L'Estrade ET, Hansen HD, Falk-Petersen C, Haugaard A, Griem-Krey N, Jung S, Lüddens H, Schirmeister T, Erlandsson M, Ohlsson T, Knudsen GM, Herth MM, Wellendorph P, Frølund B. Synthesis and Pharmacological Evaluation of [(11)C]4-Methoxy-N-[2-(thiophen-2-yl)imidazo[1,2-a]pyridin-3-yl]benzamide as a Brain Penetrant PET Ligand Selective for the δ-Subunit-Containing γ-Aminobutyric Acid Type A Receptors. ACS Omega 4: 8846-8851 (2019).

Lie ME, Gowing EK, Johansen NB, Dalby NO, Thiesen L, Wellendorph P, Clarkson AN. GAT3 selective substrate l-isoserine upregulates GAT3 expression and increases functional recovery after a focal ischemic stroke in mice. J. Cereb. Blood Flow Metab. 39: 74-88 (2019).

Liu X, Xu X, Hilger D, Aschauer P, Tiemann JKS, Du Y, Liu H, Hirata K, Sun X, Guixà-González R, Mathiesen JM, Hildebrand PW, Kobilka BK. Structural Insights into the Process of GPCR-G Protein Complex Formation. Cell 177: 1243-1251 (2019).

Malfacini, D., J. Patt, S. Annala, K. Harpsøe, F. Eryilma, R. Reher, M. Crusemann, W. Hanke, H. Zhang, D. Tietze, D.E. Gloriam, H. Bräuner-Osborne, K. Strømgaard, G.M. König, A. Inoue, J. Gomeza and E. Kostenis. Rational design of a heterotrimeric G protein alpha subunit with artificial inhibitor sensitivity. J. Biol. Chem. 294: 5747-5758 (2019).

Mos I, Jacobsen SE, Foster SR, Bräuner-Osborne H. Calcium-Sensing Receptor Internalization Is β-Arrestin-Dependent and Modulated by Allosteric Ligands. Mol. Pharmacol. 96: 463-474 (2019).

Nøhr AC, Shehata MA, Palmer D, Pokhrel R, Vallianou M, Foster SR, Gentry PR, Gloriam DE, Bräuner-Osborne H. Identification of a novel scaffold for a small molecule GPR139 receptor agonist. Sci. Rep. 9: 3802 (2019).

Poulie CBM, Alcaide A, Krell-Jørgensen M, Larsen Y, Astier E, Bjørn-Yoshimoto WE, Yi F, Syrenne JT, Storgaard M, Nielsen B, Frydenvang KA, Jensen AA, Hansen KB, Pickering DS, Bunch L. Design and Synthesis of 2,3- trans-Proline Analogues as Ligands for Ionotropic Glutamate Receptors and Excitatory Amino Acid Transporters. ACS Chem. Neurosci. 10: 2989-3007 (2019).

Sainas S, Temperini P, Farnsworth JC, Yi F, Møllerud S, Jensen AA, Nielsen B, Passoni A, Kastrup JS, Hansen KB, Boschi D, Pickering DS, Clausen RP, Lolli ML. Use of the 4-Hydroxytriazole Moiety as a Bioisosteric Tool in the Development of Ionotropic Glutamate Receptor Ligands. J. Med. Chem. 62: 4467-4482 (2019).

Thiesen L, Frølund B, Wellendorph P. Lack of evidence for synaptic high-affinity γ-hydroxybutyric acid (GHB) transport in rat brain synaptosomes and 11 Na(+) -dependent SLC neurotransmitter transporters. J. Neurochem. 149: 195-210 (2019).

Xiong, X. F., H. Zhang, M.W. Boesgaard, C.R. Underwood, H. Bräuner-Osborne and K. Strømgaard. Structure-activity relationship studies of the natural product Gq/11 protein inhibitor YM-254890. ChemMedChem 14: 865-870 (2019).

van Hout M, Valdes A, Christensen SB, Tran PT, Watkins M, Gajewiak J, Jensen AA, Olivera BM, McIntosh JM. α-Conotoxin VnIB from Conus ventricosus is a potent and selective antagonist of α6β4* nicotinic acetylcholine receptors. Neuropharmacology 157: 107691 (2019).

Wu P, Bjørn-Yoshimoto WE, Staudt M, Jensen AA, Bunch L. Identification and Structure-Activity Relationship Study of Imidazo[1,2-a]pyridine-3-amines as First Selective Inhibitors of Excitatory Amino Acid Transporter Subtype 3 (EAAT3). ACS Chem. Neurosci. 10: 4414-4429 (2019).

Zlotos DP, Mohsen AMY, Mandour YM, Marzouk MA, Breitinger U, Villmann C, Breitinger HG, Sotriffer C, Jensen AA, Holzgrabe U. 11-Aminostrychnine and N-(Strychnine-11-yl)propionamide: Synthesis, Configuration, and Pharmacological Evaluation at Glycine Receptors. J. Nat. Prod. 82: 2332-2336 (2019).

2018

Al-Khawaja A, Haugaard AS, Marek A, Löffler R, Thiesen L, Santiveri M, Damgaard M, Bundgaard C, Frølund B, Wellendorph P. Pharmacological Characterization of [(3)H]ATPCA as a Substrate for Studying the Functional Role of the Betaine/GABA Transporter 1 and the Creatine Transporter. ACS Chem. Neurosci. 9: 545-554 (2018).

Amat-Foraster M, Jensen AA, Plath N, Herrik KF, Celada P, Artigas F. Temporally dissociable effects of ketamine on neuronal discharge and gamma oscillations in rat thalamo-cortical networks. Neuropharmacology. 137: 13-23 (2018).

Crestey F, Jensen AA, Soerensen C, Magnus CB, Andreasen JT, Peters GHJ, Kristensen JL. Dual Nicotinic Acetylcholine Receptor α4β2 Antagonists/α7 Agonists: Synthesis, Docking Studies, and Pharmacological Evaluation of Tetrahydroisoquinolines and Tetrahydroisoquinolinium Salts. J. Med. Chem. 61: 1719-1729 (2018).

Elnagar MR, Walls AB, Helal GK, Hamada FM, Thomsen MS, Jensen AA. Functional characterization of α7 nicotinic acetylcholine and NMDA receptor signaling in SH-SY5Y neuroblastoma cells in an ERK phosphorylation assay. Eur J. Pharmacol. 826: 106-113 (2018).

Fu H, Zhang J, Tepper PG, Bunch L, Jensen AA, Poelarends GJ. Chemoenzymatic synthesis and pharmacological characterization of functionalized aspartate analogues as novel excitatory amino acid transporter inhibitors. J. Med. Chem. 61: 7741-7753 (2018).

Gabe, M.B.N., A.H. Sparre-Ulrich, M.F. Pedersen, L.S. Gasbjerg, A. Inoue, H. Bräuner-Osborne, B. Hartmann and M.M. Rosenkilde. Human GIP(3-30)NH2 inhibits G protein-dependent as well as G protein-independent signaling and is selective for the GIP receptor with high-affinity binding to primate but not rodent GIP receptors. Biochem. Pharmacol. 150: 97-107 (2018).

Madjroh N, Olander ER, Bundgaard C, Söderhielm PC, Jensen AA. Functional properties and mechanism of action of PPTQ, an allosteric agonist and low nanomolar positive allosteric modulator at GABAA receptors. Biochem. Pharmacol. 147:153-169 (2018).

Lie ME, Gowing EK, Clausen RP, Wellendorph P, Clarkson AN. Inhibition of GABA transporters fails to afford significant protection following focal cerebral ischemia. J. Cereb. Blood Flow Metab. 38:166-173 (2018).

Olander ER, Madjroh N, Bunch L, Söderhielm PC, Jensen AA. Delineation of the functional properties and the mechanism of action of AA29504, an allosteric agonist and positive allosteric modulator of GABAA receptors. Biochem. Pharmacol. 150: 305-319 (2018).

Peng Y, McCorvy JD, Harpsøe K, Lansu K, Yuan S, Popov P, Qu L, Pu M, Che T, Nikolajsen LF, Huang XP, Wu Y, Shen L, Bjørn-Yoshimoto WE, Ding K, Wacker D, Han GW, Cheng J, Katritch V, Jensen AA, Hanson MA, Zhao S, Gloriam DE, Roth BL, Stevens RC, Liu ZJ. 5-HT2C Receptor Structures Reveal the Structural Basis of GPCR Polypharmacology. Cell. 172: 719-730 (2018).

Polovinkin L, Hassaine G, Perot J, Neumann E, Jensen AA, Lefebvre SN, Corringer PJ, Neyton J, Chipot C, Dehez F, Schoehn G, Nury H. Conformational transitions of the serotonin 5-HT3 receptor. Nature. 563: 275-279 (2018).

Söderhielm PC, Klein AB, Bomholtz SH, Jensen AA. Profiling of GABAA and GABAB receptor expression in the myometrium of the human uterus. Life Sci. 214: 145-152 (2018).

Zhang, H. , A. Nielsen, M.W. Boesgaard, K. Harpsøe, N.L. Daly, X.-F. Xiong, C.R. Underwood, L. M. Haugaard-Kedström, H. Bräuner-Osborne, D.E. Gloriam, K. Strømgaard. Structure–activity relationship and conformational studies of the natural product cyclic depsipeptides YM-254890 and FR900359. Eur J. Med. Chem. 156: 847-860 (2018).

2017

Bader BM, Steder A, Klein AB, Frølund B, Schroeder OHU, Jensen AA. Functional characterization of GABAA receptor-mediated modulation of cortical neuron network activity in microelectrode array recordings. PLoS One. 12: e0186147 (2017).

Christensen, H.B., D.E. Gloriam, D.S. Pedersen, J.B. Cowland, N. Borregaard and H. Bräuner-Osborne. Applying label-free dynamic mass redistribution assay for studying endogenous FPR1 receptor signaling in human neutrophils. J. Pharmacol. Toxicol. Methods 88: 72-78 (2017).

Clemmensen, C., C.V. Jørgensen, S. Smajilovic and H. Bräuner-Osborne. Robust GLP-1 secretion by basic L-amino acids does not require the GPRC6A receptor. Diabetes Obes. Metab. 19: 599-603 (2017).

Damgaard M, Al-Khawaja A, Nittegaard-Nielsen M, Petersen RF, Wellendorph P and Frølund B. Monastrol, a 3,4-dihydropyrimidin-2(1H)-thione, as structural scaffold for the development of modulators for GHB high-affinity binding sites and α1β2δ GABAA receptors. Eur. J. Med. Chem. 138: 300-312 (2017).

Elnagar MR, Walls AB, Helal GK, Hamada FM, Thomsen MS, Jensen AA. Probing the putative α7 nAChR/NMDAR complex in human and murine cortex and hippocampus: Different degrees of complex formation in healthy and Alzheimer brain tissue. PLoS One. 12:e0189513 (2017).

Falk-Petersen CB, Søgaard R, Madsen KL, Klein AB, Frølund B and Wellendorph P. Development of a Robust Mammalian Cell-based Assay for Studying Recombinant α4β1/3δ GABAA Receptor Subtypes. Basic Clin. Pharmacol. Toxicol. 121 :119-129 (2017).

Frandsen, I.O., M.W. Boesgaard , K. Fidom, A. Hauser, V. Isberg, H. Bräuner-Osborne, P. Wellendorph and D.E. Gloriam. Identification of histamine H3 receptor ligands using a new crystal structure fragment-based method. Sci. Rep. 7: 4829 (2017).

Harpsøe, K., M.W. Boesgaard, C. Munk, H. Bräuner-Osborne and D.E. Gloriam. Structural insight to mutagenesis effects uncover a common allosteric site within class C GPCRs. Bioinformatics 33: 1116-1120 (2017).

Jacobsen S.E., I. Ammendrup-Johnsen , A.M. Jansen, U. Gether, K.L. Madsen and H. Bräuner-Osborne. The GPRC6A receptor displays constitutive internalization and is being sorted to the slow recycling pathway. J. Biol. Chem. 292: 6910-6926 (2017).

Jacobsen S.E., U. Gether and H. Bräuner-Osborne. Investigating the molecular mechanism of positive and negative allosteric modulators in the calcium-sensing receptor dimer. Sci. Rep. 7: 46355 (2017).

Jensen, A.A., J.D. McCorvy, S. Leth-Petersen, C. Bundgaard, G. Liebscher, T.P. Kenakin, H. Bräuner-Osborne, J. Kehler and J.L. Kristensen. Detailed characterization of the in vitro pharmacological and pharmacokinetic properties of N-(2-hydroxybenzyl)-2,5-dimethyl-4-cyanophenylethylamine (25CN-NBOH), a highly selective and brain-penetrant 5-HT2A receptor agonist. J. Pharmacol. Exp. Ther. 361: 441-453 (2017).

Jensen CH, Hansen HD, Bay T, Vogensen SB, Lehel S, Thiesen L, Bundgaard C, Clausen RP, Knudsen GM, Herth MM, Wellendorph P, Frølund B. Radiosynthesis and Evaluation of [11C]3-Hydroxycyclopent-1-enecarboxylic Acid as Potential PET Ligand for the High-Affinity γ-Hydroxybutyric Acid Binding Sites. ACS Chem. Neurosci. 8: 22-27 (2017).

Jepsen TH, Glibstrup E, Crestey F, Jensen AA, Kristensen JL. A strategic approach to [6,6]-bicyclic lactones: application towards the CD fragment of DHβE. Beilstein J. Org. Chem. 13: 988-994 (2017).

Jessen, M., K. Frederiksen, F. Yi, R.P. Clausen, K.B. Hansen, H. Bräuner-Osborne, P. Kliburn and A. Damholt. Identification of AICP as a GluN2C-selective NMDA receptor superagonist at the GluN1 glycine site. Mol. Pharmacol. 92: 151-161 (2017).

Jørgensen, L., A. Al-Khawaja, S. Kickinger, S.B. Vogensen, J. Skovgaard-Petersen, E.R. Jensen, N. Borkar, R. Löffler, K.K. Madsen, H. Bräuner-Osborne, A. Schousboe, G.F. Ecker, P. Wellendorph and R.P. Clausen. Structure-activity relationship, pharmacological characterization and molecular modeling of non-competitive inhibitors of the betaine/γ-aminobutyric acid transporter 1 (BGT1). J. Med. Chem. 60: 8834-8846 (2017).

Jørgensen S, Have CT, Underwood CR, Johansen LD, Wellendorph P, Gjesing AP, Jørgensen CV, Quan S, Rui G, Inoue A, Linneberg A, Grarup N, Jun W, Pedersen O, Hansen T, Bräuner-Osborne H. Genetic Variations in the Human G Protein-coupled Receptor Class C, Group 6, Member A (GPRC6A) Control Cell Surface Expression and Function. J. Biol. Chem. 292: 1524-1534 (2017).

Krall J, Jensen CH, Bavo F, Falk-Petersen CB, Haugaard AS, Vogensen SB, Tian Y, Nittegaard-Nielsen M, Sigurdardóttir SB, Kehler J, Kongstad KT, Gloriam DE, Clausen RP, Harpsøe K, Wellendorph P, Frølund B. Molecular Hybridization of Potent and Selective γ-Hydroxybutyric Acid (GHB) Ligands: Design, Synthesis, Binding Studies, and Molecular Modeling of Novel 3-Hydroxycyclopent-1-enecarboxylic Acid (HOCPCA) and trans-γ-Hydroxycrotonic Acid (T-HCA) Analogs. J. Med. Chem. 60: 9022-9039 (2017).

Lie MEK, Al-Khawaja A, Damgaard M, Haugaard AS, Schousboe A, Clarkson AN, Wellendorph P. Glial GABA Transporters as Modulators of Inhibitory Signalling in Epilepsy and Stroke. Adv. Neurobiol. 16:137-167 (2017).

Nøhr, A.C., W. Jespers, M.A. Shehata, L. Floryan, V. Isberg, K.B. Andersen, J. Åqvist, H. Guyiérrez-de-Terán, H. Bräuner-Osborne and D.E. Gloriam. The GPR139 reference agonists 1a and 7c, and tryptophan and phenylalanine share a common binding site. Sci. Rep. 1128 (2017).

Nøhr, A.C., M.A. Shehata, A.S. Hauser, V. Isberg, J. Mokrosinski, I.S. Farooqi, D.S. Pedersen, D.E. Glorium and H. Bräuner-Osborne. The orphan G protein-coupled receptor GPR139 is activated by the peptides: adrenocorticotropic hormone (ACTH), α-, and β-melanocyte stimulating hormone (α- MSH, and β-MSH), and the conserved core motif HFRW. Neurochem. Int. 102: 105-113 (2017).

Petersen IN, Villadsen J, Hansen HD, Madsen J, Jensen AA, Gillings N, Lehel S, Herth MM, Knudsen GM, Kristensen JL. 18F-Labelling of electron rich iodonium ylides: application to the radiosynthesis of potential 5-HT2A receptor PET ligands. Org. Biomol. Chem. 15:4351-4358 (2017).

Roszko K., R. Bi, C. Gorvin, H. Bräuner-Osborne, X. Xiong, A. Innoue, R. Thakker, K. Strømgaard, T. Gardella and M. Mannstadt. Knock-in mouse with mutant Gα11 mimics human inherited hypocalcemia and is rescued by pharmacologic inhibitors. JCI Insight 2: e91079 (2017).

Schousboe A, Wellendorph P, Frølund B, Clausen RP, Krogsgaard-Larsen P. Astrocytic GABA Transporters: Pharmacological Properties and Targets for Antiepileptic Drugs. Adv. Neurobiol. 16:283-296 (2017).

Zhang, H., X.-F. Xiong, M.W. Boesgaard, C.R. Underwood, H. Bräuner-Osborne and K. Strømgaard. Structure-activity relationship studies of the cyclic depsipeptide natural product YM-254890 targeting the Gq protein. ChemMedChem 12: 830-834 (2017).

2016

Chua HC, Christensen ET, Hoestgaard-Jensen K, Hartiadi LY, Ramzan I, Jensen AA, Absalom NL, Chebib M. Kavain, the Major Constituent of the Anxiolytic Kava Extract, Potentiates GABAA Receptors: Functional Characteristics and Molecular Mechanism. PLoS One. 11:e0157700 (2016).

Clausen RP, Mohr AØ, Riise E, Jensen AA, Gill A, Madden DR, Kastrup JS, Skottrup PD. A parallel panning scheme used for selection of a GluA4-specific Fab targeting the ligand-binding domain. Int. J. Biol. Macromol. 92:779-787 (2016).

Gasiorek A, Trattnig SM, Ahring PK, Kristiansen U, Frølund B, Frederiksen K, Jensen AA. Delineation of the functional properties and the mechanism of action of TMPPAA, an allosteric agonist and positive allosteric modulator of 5-HT3 receptors. Biochem. Pharmacol. 110-111:92-108 (2016).

Hansen JC, Bjørn-Yoshimoto WE, Bisballe N, Nielsen B, Jensen AA, Bunch L. β-Sulfonamido Functionalized Aspartate Analogues as Excitatory Amino Acid Transporter Inhibitors: Distinct Subtype Selectivity Profiles Arising from Subtle Structural Differences. J Med Chem. 59:8771-8786 (2016).

Hansen SW, Erichsen MN, Huynh TH, Ruiz JA, Haym I, Bjørn-Yoshimoto WE, Abrahamsen B, Hansen J, Storgaard M, Eriksen AL, Jensen AA, Bunch L. New Insight into the Structure-Activity Relationships of the Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitors UCPH-101 and UCPH-102. ChemMedChem. 11:382-402 (2016).

Hansen SW, Erichsen MN, Fu B, Bjørn-Yoshimoto WE, Abrahamsen B, Hansen JC, Jensen AA, Bunch L. Identification of a New Class of Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitors Followed by a Structure-Activity Relationship Study. J Med Chem. 59:8757-8770 (2016).

Haym I, Huynh TH, Hansen SW, Pedersen MH, Ruiz JA, Erichsen MN, Gynther M, Bjørn-Yoshimoto WE, Abrahamsen B, Bastlund JF, Bundgaard C, Eriksen AL, Jensen AA, Bunch L. Bioavailability Studies and in vitro Profiling of the Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitor UCPH-102. ChemMedChem. 11:403-19 (2016).

Herth MM, Petersen IN, Hansen HD, Hansen M, Ettrup A, Jensen AA, Lehel S, Dyssegaard A, Gillings N, Knudsen GM, Kristensen JL. Synthesis and evaluation of 18F-labeled 5-HT2A receptor agonists as PET ligands. Nucl. Med. Biol. 43:455-462 (2016).

Klein AB, Bay T, Villumsen IS, Falk-Petersen CB, Marek A, Frølund B, Clausen RP, Hansen HD, Knudsen GM, Wellendorph P. Autoradiographic imaging and quantification of the high-affinity GHB binding sites in rodent brain using 3H-HOCPCA. Neurochem Int. 100:138-145 (2016).

Klein AB, Nittegaard-Nielsen M, Christensen JT, Al-Khawaja A, Wellendorph P. Demonstration of the dynamic mass redistribution label-free technology as a useful cell-based pharmacological assay for endogenously expressed GABAA receptors. MedChemComm. 7:426–32 (2016).

Krall J, Brygger BM, Sigurðardóttir SB, Ng CK, Bundgaard C, Kehler J, Nielsen B, Bek T, Jensen AA, Frølund B. Discovery of α-Substituted Imidazole-4-acetic Acid Analogues as a Novel Class of ρ(1) γ-Aminobutyric Acid Type A Receptor Antagonists with Effect on Retinal Vascular Tone. ChemMedChem. 11:2299-2310 (2016).

Kuhne S., A.C. Nøhr, A. Marek, T. Elbert, A.B. Klein, H. Bräuner-Osborne, P. Wellendorph and D.S. Pedersen. Radiosynthesis and characterization of a potent and selective GPR139 agonist radioligand. RCS Adv. 6: 947-952 (2016).

Mohsen AM, Mandour YM, Sarukhanyan E, Breitinger U, Villmann C, Banoub MM, Breitinger HG, Dandekar T, Holzgrabe U, Sotriffer C, Jensen AA, Zlotos DP. Oxime Ethers of (E)-11-Isonitrosostrychnine as Highly Potent Glycine Receptor Antagonists. J. Nat. Prod. 79: 2997-3005 (2016).

Petersen IN, Villadsen J, Hansen HD, Jensen AA, Lehel S, Gillings N, Herth MM, Knudsen GM, Kristensen JL. Convergent 18F-labeling and evaluation of N-benzyl-phenethylamines as 5-HT2A receptor PET ligands. Bioorg Med Chem. 24:5353-5356 (2016).

Shehata, M.A., A.C. Nøhr, D. Lissa, C. Bisig, V. Isberg, K.B. Andersen, K. Harpsøe, F. Bjørkling,  H. Bräuner-Osborne and D.E. Gloriam. Novel agonist bioisosteres and common structure-activity relationships for the orphan G protein-coupled receptor GPR139. Sci. Rep. 6: 36681 (2016).

Trattnig SM, Gasiorek A, Deeb TZ, Ortiz EJ, Moss SJ, Jensen AA, Davies PA. Copper and protons directly activate the zinc-activated channel. Biochem. Pharmacol. 103:109-17 (2016).

Wang SY, Larsen Y, Navarrete CV, Jensen AA, Nielsen B, Al-Musaed A, Frydenvang K, Kastrup JS, Pickering DS, Clausen RP. Tweaking Subtype Selectivity and Agonist Efficacy at (S)-2-Amino-3-(3-hydroxy-5-methyl-isoxazol-4-yl)propionic acid (AMPA) Receptors in a Small Series of BnTetAMPA Analogues. J. Med. Chem. 59:2244-54 (2016).

Xiong XF, Zhang H, Underwood CR, Harpsøe K, Gardella TJ, Wöldike MF, Mannstadt M, Gloriam DE, Bräuner-Osborne H, Strømgaard K. Total synthesis and structure-activity relationship studies of a series of selective G protein inhibitors. Nature Chem. 8:1035-1041 (2016).

2015

Bach TB, Jensen AA, Petersen JG, Sørensen TE, Della Volpe S, Liu J, Blaazer AR, van Muijlwijk-Koezen JE, Balle T, Frølund B. Exploration of the molecular architecture of the orthosteric binding site in the α4β2 nicotinic acetylcholine  receptor with analogs of 3-(dimethylamino)butyl dimethylcarbamate (DMABC) and 1-(pyridin-3-yl)-1,4-diazepane. Eur. J. Med. Chem. 102: 425-44 (2015).

Damgaard M, Al-Khawaja A, Vogensen SB, Jurik A, Sijm M, Lie ME, Bæk MI, Rosenthal E, Jensen AA, Ecker GF, Frølund B, Wellendorph P, Clausen RP. Identification of the First Highly Subtype-Selective Inhibitor of Human GABA Transporter GAT3. ACS Chem. Neurosci. 6: 1591-9 (2015).

de la Fuente Revenga M, Balle T, Jensen AA, Frølund B. Conformationally restrained carbamoylcholine homologues. Synthesis, pharmacology at neuronal nicotinic acetylcholine receptors and biostructural considerations. Eur. J. Med. Chem. 102: 352-62 (2015).

Fisher PM, Holst KK, Adamsen D, Klein AB, Frokjaer VG, Jensen PS, Svarer C, Gillings N, Baare WF, Mikkelsen JD, Knudsen GM. BDNF Val66met and 5-HTTLPR polymorphisms predict a human in vivo marker for brain serotonin levels. Hum. Brain Mapp. 36: 313-23 (2015).

Grupe M, Grunnet M, Bastlund JF, Jensen AA. Targeting α4β2 Nicotinic Acetylcholine Receptors in Central Nervous System Disorders: Perspectives on Positive Allosteric Modulation as a Therapeutic Approach. Basic Clin. Pharmacol. Toxicol. 116: 187-200 (2015).

Hammer H, Bader BM, Ehnert C, Bundgaard C, Bunch L, Hoestgaard-Jensen K, Schroeder OH, Bastlund JF, Gramowski-Voß A, Jensen AA. A Multifaceted GABAA Receptor Modulator: Functional Properties and Mechanism of Action of the Sedative-Hypnotic and Recreational Drug Methaqualone (Quaalude). Mol. Pharmacol. 88: 401-420 (2015).

Hammer H, Ebert B, Jensen HS, Jensen AA. Functional characterization of the 1,5-benzodiazepine clobazam and its major active metabolite N-desmethylclobazam at human GABA(A) receptors expressed in Xenopus laevis oocytes. PLoS One. 10: e0120239 (2015).

Hansen, M., S.E. Jacobsen, S. Plunkett, G.E. Liebscher, J.D. McCorvy, H. Bräuner-Osborne and J.L. Kristensen, Synthesis and pharmacological evaluation of N-benzyl substituted 4-bromo-2,5-dimethoxyphenethylamines as 5-HT2A/2C partial agonists. Bioorg. Med. Chem. 23: 3933-3937 (2015).

Harpsøe K, Isberg V, Tehan BG, Weiss D, Arsova A, Marshall FH, Bräuner-Osborne H, Gloriam DE. Selective Negative Allosteric Modulation Of Metabotropic Glutamate Receptors - A Structural Perspective of Ligands and Mutants. Sci. Rep. 5: 13869 (2015).

Jensen AA, Fahlke C, Bjørn-Yoshimoto WE, Bunch L. Excitatory amino acid transporters: recent insights into molecular mechanisms, novel modes of modulation and new therapeutic possibilities. Curr. Opin. Pharmacol. 20: 116-123 (2015).

Johansson H., Boesgaard M.W., Norskov-Lauritsen L., Larsen I., Kuhne S., Gloriam D.E., Brauner-Osborne H. and Sejer Pedersen D., Selective allosteric antagonists for the G protein-coupled receptor GPRC6A based on the 2-phenylindole privileged structure scaffold. J. Med. Chem. 58: 8938-8951 (2015).

Lund, T.M., K.B. Ploug, A. Iversen, A.A. Jensen, and I. Jansen-Olesen. The metabolic impact of β-hydroxybutyrate on neurotransmission: Reduced glycolysis mediates changes in calcium responses and KATP receptor sensitivity. J. Neurochem. 132:520-531 (2015).

Nørskov-Lauritsen L, Bräuner-Osborne H. Role of post-translational modifications on structure, function and pharmacology of class C G protein-coupled receptors. Eur. J. Pharmacol. 763: 233-40 (2015).

Nørskov-Lauritsen L, Jørgensen S, Bräuner-Osborne H. N-glycosylation and disulfide bonding affects GPRC6A receptor expression, function, and dimerization. FEBS Lett. 589: 588-597 (2015).

Pedraz-Cuesta E, Christensen S, Jensen AA, Jensen NF, Bunch L, Romer MU, Brünner N, Stenvang J, Pedersen SF. The glutamate transport inhibitor DL-Threo-β-Benzyloxyaspartic acid (DL-TBOA) differentially affects SN38- and oxaliplatin-induced death of drug-resistant colorectal cancer cells. BMC Cancer.  15: 411 (2015).

Petersen IN, Crestey F, Jensen AA, Indurthi DC, Pedersen H, Andreasen JT, Balle T, Kristensen JL. Tying up Nicotine: New Selective Competitive Antagonist of the Neuronal Nicotinic Acetylcholine Receptors. ACS Med Chem Lett. 6:472-475 (2015).

Roed SN, Nøhr AC, Wismann P, Iversen H, Bräuner-Osborne H, Knudsen SM, Waldhoer M. Functional consequences of glucagon-like peptide-1 receptor cross-talk and trafficking. J. Biol. Chem. 290: 1233-43 (2015).

Shehata, M.A., H.B. Christensen, V. Isberg, D.S. Pedersen, A. Bender, H. Bräuner-Osborne and D.E. Gloriam. Identification of the first surrogate agonists for the G protein-coupled receptor GPR132. RSC Advances 5: 48551-48557 (2015).

Thiesen L, Kehler J, Clausen RP, Frølund B, Bundgaard C, Wellendorph P. In Vitro and In Vivo Evidence for Active Brain Uptake of the GHB Analog HOCPCA by the Monocarboxylate Transporter Subtype 1. J. Pharmacol. Exp. Ther. 354: 166-174 (2015).

Vedel, L., H. Bräuner-Osborne and J.M. Mathiesen. A cAMP biosensor-based High Throughput Screening assay for identification of Gs-coupled GPCR ligands and phosphodiesterase inhibitors. J. Biomol. Screen. 20: 849-857 (2015).

Villumsen IS, Wellendorph P, Smart TG. Pharmacological characterisation of murine α4β1δ GABA-A receptors expressed in Xenopus oocytes. BMC Neurosci. 16: 8 (2015).

Visser AK, Ettrup A, Klein AB, van Waarde A, Bosker FJ, Meerlo P, Knudsen GM,  de Boer SF. Similar serotonin-2A receptor binding in rats with different coping styles or levels of aggression. Synapse. 69: 226-232 (2015).

2014

Adelfinger L, Turecek R, Ivankova K, Jensen AA, Moss SJ, Gassmann M, Bettler B.GABAB receptor phosphorylation regulates KCTD12-induced K+ current desensitization. Biochem. Pharmacol. 91: 369-379 (2014).

Al-Khawaja, A., J.G. Petersen, M. Damgaard, M.H. Jensen, S. Vogensen, M. Lie, B. Kragholm, H. Bräuner-Osborne, R.P. Clausen, B. Frølund and P. Wellendorph. Pharmacological identification of a guanidine-containing β-alanine analogue with low micromolar potency and selectivity for the betaine/GABA transporter 1 (BGT1). Neurochem. Res. 39: 1988-1996 (2014).

Bay T, Eghorn LF, Klein AB, Wellendorph P. GHB receptor targets in the CNS: Focus on high-affinity binding sites. Biochem. Pharmacol. 87: 220-228 (2014).

Clemmensen, C., S. Smajilovic, P. Wellendorph and H. Bräuner-Osborne. The GPRC6A receptor: From cloning to physiological function. Br. J. Pharmacol. 171: 1129-1141 (2014).

Eghorn LF, Hoestgaard-Jensen K, Kongstad KT, Bay T, Higgins D, Frølund B, Wellendorph P. Positive allosteric modulation of the GHB high-affinity binding site by the GABAA receptor modulator monastrol and the flavonoid catechin. Eur. J. Pharmacol. 740: 570-577 (2014).

Erichsen MN, Hansen J, Ruiz JA, Demmer CS, Abrahamsen B, Bastlund JF, Bundgaard C, Jensen AA, Bunch L. Probing for Improved Potency and In Vivo Bioavailability of Excitatory Amino Acid Transporter Subtype 1 Inhibitors UCPH-101 and UCPH-102: Design, Synthesis and Pharmacological Evaluation of Substituted 7-Biphenyl Analogs. Neurochem. Res. 39: 1964-79 (2014).

Hansen, M., K. Phonekeo, J. Paine, S. Leth-Hansen, M. Begtrup, H. Bräuner-Osborne and J. Kristensen. Synthesis and structure-activity relationships of N-benzyl phenethylamines as 5-HT2A/2C agonists. ACS Chem. Neurosci. 5: 243-249 (2014).

Hoestgaard-Jensen K, Dalby NO, Krall J, Hammer H, Krogsgaard-Larsen P, Frølund B, Jensen AA. Probing α4βδ GABAA Receptor Heterogeneity: Differential Regional Effects of a Functionally Selective α4β1δ/α4β3δ Receptor Agonist on Tonic and Phasic Inhibition in Rat Brain. J Neurosci. 34: 16256-72 (2014).

Isberg, V., K.B. Andersen, C. Bisig, G.P.H. Dietz, H. Bräuner-Osborne and D.E. Gloriam. Computer-aided discovery of aromatic L-α-amino acids as agonists of the orphan G protein-coupled receptor GPR139. J. Chem. Inf. Model.  54: 1553-1557 (2014).

Jensen AB, Hoestgaard-Jensen K, Jensen AA. Pharmacological characterisation of α6β4(⁎) nicotinic acetylcholine receptors assembled from three chimeric α6/α3 subunits in tsA201 cells. Eur. J. Pharmacol. 740: 703-713 (2014).

Jepsen TH, Jensen AA, Lund MH, Glibstrup E, Kristensen JL. Synthesis and Pharmacological Evaluation of DHβE Analogues as Neuronal Nicotinic Acetylcholine Receptor Antagonists. ACS Med Chem Lett. 5: 766-770 (2014).

Klein AB, Ultved L, Adamsen D, Santini MA, Tobeña A, Fernandez-Teruel A, Flores P, Moreno M, Cardona D, Knudsen GM, Aznar S, Mikkelsen JD. 5-HT2A and mGlu2 receptor binding levels are related to differences in impulsive behavior in the Roman Low- (RLA) and High- (RHA) avoidance rat strains. Neuroscience. 263: 36-45 (2014).

Krall J, Kongstad KT, Nielsen B, Sørensen TE, Balle T, Jensen AA, Frølund B. 5-(Piperidin-4-yl)-3-Hydroxypyrazole: A Novel Scaffold for Probing the Orthosteric γ-Aminobutyric Acid Type A Receptor Binding Site. ChemMedChem. 9:2475-85 (2014).

Krogsgaard-Larsen N, Jensen AA, Schrøder TJ, Christoffersen CT, Kehler J. Novel Aza-analogous Ergoline Derived Scaffolds as Potent Serotonin 5-HT6 and Dopamine D2 Receptor Ligands. J. Med. Chem. 57: 5823-5828 (2014).

Mohsen AM, Heller E, Holzgrabe U, Jensen AA, Zlotos DP. Structure-activity relationships of strychnine analogs at glycine receptors. Chem. Biodivers. 11: 1256-1262 (2014).

Mølck, C., K. Harpsøe, D.E. Gloriam, J.M. Mathiesen, S.M. Nielsen and H. Bräuner-Osborne. mGluR5: Exploration of orthosteric and allosteric ligand binding pockets and their applications to drug discovery. Neurochem. Res. 39: 1862-1875 (2014).

Nørskov-Lauritsen, L., A.R.B. Thomsen and H. Bräuner-Osborne. G protein-coupled receptor signaling analysis using assays homogenous time-resolved Förster resonance energy transfer (HTRF®) technology. Int. J. Mol. Sci. 15: 2554-2572 (2014).

Petersen JG, Sørensen T, Damgaard M, Nielsen B, Jensen AA, Balle T, Bergmann R, Frølund B. Synthesis and pharmacological evaluation of 6-aminonicotinic acid analogues as novel GABAA receptor agonists. Eur. J. Med. Chem. 84C: 404-416 (2014).

Pinto A, Tamborini L, Mastronardi F, Ettari R, Safoz Y, Bunch L, Nielsen B, Jensen AA, De Micheli C, Conti P. Synthesis of (3-hydroxy-pyrazolin-5-yl)glycine based ligands interacting with ionotropic glutamate receptors. Eur. J. Med. Chem. 75C: 151-158 (2014).

Pyndt Jørgensen B, Hansen JT, Krych L, Larsen C, Klein AB, Nielsen DS, Josefsen K, Hansen AK, Sørensen DB. A Possible Link between Food and Mood: Dietary Impact on Gut Microbiota and Behavior in BALB/c Mice. PLoS One. 9: e103398 (2014).

Roed, S.N., P. Wismann, C.R. Underwood, N. Kulahin, H. Iversen, K.A. Cappelen, L. Schäffer, J. Lehtonen, J. Hecksher-Soerensen, A. Secher, J.M. Mathiesen, H. Bräuner-Osborne, J.L. Whistler, S.M. Knudsen and M. Waldhoer. Real-time trafficking and signaling of the glucagon-like peptide-1 receptor. Mol. Cell. Endocrinolol. 382: 938-949 (2014).

Ryan KK, V Tremaroli, C. Clemmensen, P Kovatcheva-Datchary, A Myronovych, R Karns, HE Wilson-Pérez, DA Sandoval, R Kohli, F Bäckhed and RJ Seeley. FXR is a molecular target for the effects of vertical sleeve gastrectomy. Nature. 509:183-188 (2014).

Smajilovic, S., P. Wellendorph and H. Bräuner-Osborne. Promiscuous seven transmembrane receptors sensing L-α-amino acids. Curr. Pharm. Design. 20: 2693-2702 (2014).

Zlotos DP, Tränkle C, Holzgrabe U, Gündisch D, Jensen AA. Semisynthetic analogues of toxiferine I and their pharmacological properties at α7 nAChRs, muscle-type nAChRs, and the allosteric binding site of muscarinic M2 receptors. J. Nat. Prod. 77:2006-13 (2014).

2013

Abrahamsen B, Schneider N, Erichsen MN, Huynh TH, Fahlke C, Bunch L, Jensen AA. Allosteric modulation of an excitatory amino acid transporter: The subtype-selective inhibitor UCPH-101 exerts sustained inhibition of EAAT1 through an intramonomeric site in the trimerization domain. J. Neurosci. 33: 1068-1087 (2013).

Assaf, Z., A.P. Larsen, R. Venskutonytė, L. Han, B. Abrahamsen, B. Nielsen, M. Gajhede, J.S. Kastrup, A.A. Jensen, D.S. Pickering, K. Frydenvang, T. Gefflaut, and L. Bunch. Chemo-enzymatic synthesis of new 2,4-syn-functionalized (S)-glutamate analogues and structure-activity relationship studies at ionotropic glutamate receptors and excitatory amino acid transporters. J. Med. Chem. 28: 1614-1628 (2013).

Attia, M.I., C. Herdeis and H. Bräuner-Osborne. Synthesis and pharmacological characterization of certain baclofen analogues. Dig. J. Nanomater. Bios. 8: 139-149 (2013).

Aznar S and Klein AB. Regulating Prefrontal Cortex Activation: An Emerging Role for the 5-HT Serotonin Receptor in the Modulation of Emotion-Based Actions? Mol. Neurobiol. 48: 841-853 (2013).

Beckmann HS, Nie F, Hagerman CE, Johansson H, Tan YS, Wilcke D and Spring DR. A strategy for the diversity-oriented synthesis of macrocyclic scaffolds using multidimensional coupling. Nature Chem. 5: 861-867 (2013).

Chalikiopoulos A, Thiele S, Malmgaard-Clausen M, Rydberg P, Isberg V, Ulven T, Frimurer TM, Rosenkilde MM, Gloriam DE. Structure-activity relationships and identification of optimized CC-chemokine receptor CCR1, 5, and 8 metal-ion chelators. J. Chem. Inf. Model. 53: 2863-2873 (2013).

Clemmensen, C., C. Pehmøller, A.B. Klein, C. Ratner, J.F.P. Wojtaszewski and H. Bräuner-Osborne. Enhanced voluntary wheel running in GPRC6A receptor knockout mice. Physiol. Behavior  118: 144-151 (2013).

Clemmensen C, Smajilovic S, Madsen AN, Klein AB, Holst B, Bräuner-Osborne Increased susceptibility to diet-induced obesity in GPRC6A receptor knockout mice. H. J. Endocrinolol. 217: 151-160 (2013).

Clemmensen, C., S. Smajilovic, S.C. Woods, H. Bräuner-Osborne, R.J. Seeley, D.A. D'Alessio and K.K. Ryan. Oral L-arginine potently stimulates GLP-1 secretion to improve glucose tolerance in mice. Endocrinolol. 154: 3978-3983 (2013)

Crestey F, Jensen AA, Borch M, Andreasen JT, Andersen J, Balle T and Kristensen JL. Design, synthesis, and biological evaluation of erythrina alkaloid analogues as neuronal nicotinic acetylcholine receptor antagonists. J. Med. Chem. 56: 9673-9682 (2013).

Elfving B, Christensen T, Ratner C, Wienecke J, Klein AB. Transient activation of mTOR following forced treadmill exercise in rats. Synapse 67: 620-625 (2013).

Gloriam DE. Chemogenomics of allosteric binding sites in GPCRs. Drug Discov. Today Technol. 10: e307-313 (2013).

Grupe M, Jensen A, Ahring P, Christensen J, Grunnet M. Unravelling the mechanism of action of NS9283, a positive allosteric modulator of α43β22 nicotinic ACh receptors. Br. J. Pharmacol. 168: 2000-10 (2013).

Grupe M, Paolone G, Jensen AA, Sandager-Nielsen K, Sarter M, Grunnet M. Selective potentiation of (α4)3(β2)2 nicotinic acethylcholine receptors augments amplitudes of prefrontal acetylcholine- and nicotine-evoked glutamateric transients in rats. Biochem. Pharmacol. 86: 1487-1496 (2013).

Haagensen AM, Klein AB, Ettrup A, Matthews LR, Sørensen DB. Cognitive performance of göttingen minipigs is affected by diet in a spatial hole-board discrimination test. PLoS One. 8: e79429 (2013).

Huynh, T.H.V., C.S. Demmer, B. Abrahamsen, E. Marcher, M. Frykman, A.A. Jensen, and L. Bunch. Structure-activity-relationship study of N-acyl-N-phenylpiperazines as potential inhibitors of the excitatory amino acid transporters (EAATs): Improving the potency of a micromolar screening hit is not truism. SpringerPlus. 2:112 (2013).

Høstgaard-Jensen, K., B.C. Finger, N.O. Dalby, C. Simonsen, R.M. O'Connor, H. Hammer, M.L. Bergmann, U. Kristiansen, P. Krogsgaard-Larsen, H. Bräuner-Osborne, B. Ebert, B. Frølund, J.F. Cryan and A.A. Jensen. The orthosteric GABAA ligand Thio-4-PIOL displays distinctly different functional properties at synaptic and extrasynaptic receptors. Br. J. Pharmacol. 170: 919-932 (2013).

Isberg V, Paine J, Leth-Petersen S, Kristensen JL, Gloriam DE. Structure-activity relationships of constrained phenylethylamine ligands for the serotonin 5-HT2 receptors. PLoS One. 8: e78515 (2013).

Jacobsen, S.E., L. Nørskov-Lauritsen, A.R.B. Thomsen, S. Smajilovic, P. Wellendorph, V. K. Bhatia and H. Bräuner-Osborne. Delineation of the signaling pathways employed by the mouse GPRC6A receptor stably expressed in Chinese hamster ovary cells. J. Pharmacol. Exp. Ther. 347: 298-309 (2013).

Jensen AA, Plath N, Pedersen MH, Isberg V, Krall J, Wellendorph P, Stensbøl TB, Gloriam DE, Krogsgaard-Larsen P, Frølund B. Design, Synthesis, and Pharmacological Characterization of N- and O-Substituted 5,6,7,8-Tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol Analogues: Novel 5-HT2A/5-HT2C Receptor Agonists with Pro-Cognitive Properties. J. Med. Chem. 56: 1211-1127 (2013).

Jensen AB, Hoestgaard-Jensen K, Jensen AA. Elucidation of molecular impediments in the alpha6 subunit for in vitro expression of funcitonal alpha6beta4* nicotinic acetylcholine receptors. J. Biol. Chem. 288: 33708-33021 (2013).

Johansson H., T. Cailly, A.R.B. Thomsen, H. Bräuner-Osborne, D. Sejer Pedersen. Synthesis of the Calcilytic Ligand NPS2143. Beilstein J. Org. Chem. 9: 1383-1387 (2013).

Johansson, H., T.B. Jørgensen, D.E. Gloriam, H. Bräuner-Osborne and D.S. Pedersen. 3-Substituted 2-phenyl-indoles: Privileged structures for medicinal chemistry. RSC Advances 3: 945-960 (2013).

Jørgensen CV, Jacobsen JP, Caron MG, Klein AB, Knudsen GM and Mikkelsen JD. Cerebral 5-HT2A receptor binding, but not mGluR2, is increased in tryptophan hydrolase 2 decrease-of-function mice. Neurosci. Lett. 555: 118-122 (2013).

Jørgensen CV, Klein AB, El-Sayed M, Knudsen GM, Mikkelsen JD. Metabotropic glutamate receptor 2 and corticotrophin-releasing factor receptor-1 gene expression is differently regulated by BDNF in rat primary cortical neurons. Synapse 67:794-800 (2013).

Karim N, Wellendorph P, Absalom N, Johnston GA, Hanrahan JR, Chebib M.Potency of GABA at human recombinant GABAA receptors expressed in Xenopus oocytes: a mini
review. Amino Acids. 44: 1139-49 (2013).

Klein AB, Jennum P, Knudsen S, Gammeltoft S, Mikkelsen JD. Increased serum BDNF levels in hypocretin-deficient narcoleptic patients. Neurosci. Lett. 544: 31-5 (2013).

Kragholm, B., T. Kvist, K.K. Madsen, L. Jørgensen, S.B. Vogensen, A. Schousboe, R.P. Clausen, A.A. Jensen and H. Bräuner-Osborne. Discovery of a subtype selective inhibitor of the human betaine/GABA transporter 1 (BGT-1) with a non-competitive profile. Biochem. Pharmacol. 86: 521-528 (2013).

Krall J, Jensen CH, Sørensen TE, Nielsen B, Jensen AA, Sander T, Balle T, Frølund B. Exploring the orthosteric binding site of the γ-aminobutyric acid type A receptor using 4-(Piperidin-4-yl)-1-hydroxypyrazoles 3- or 5-imidazolyl substituted: design, synthesis, and pharmacological evaluation. J. Med. Chem. 56: 6536-6540 (2013).

Kvist, T., J.R. Greenwood, K.B. Hansen, S.F. Traynelis and H. Bräuner-Osborne. Structure-based discovery of antagonists of GluN3-containing N-methyl-D-aspartate receptors. Neuropharmacology 75: 324-336 (2013).

Kvist, T., T.B. Steffensen, J.R. Greenwood, F.M. Tabrizi, K.B. Hansen, M. Gajhede, D.S. Pickering, S.F. Traynelis, J.S. Kastrup and H. Bräuner-Osborne. Molecular mechanism of a novel NMDA receptor antagonist at the GluN1 glycine-site. J. Biol. Chem. 288: 33124-33135 (2013).

Mathiesen, J.M., L. Vedel and H. Bräuner-Osborne. cAMP biosensors applied in molecular pharmacological studies of G protein-coupled receptors. Methods Enzymol. 522: 191-208 (2013).

Pehere, A.D., M. Pietsch, M. Gütschow, P. M. Neilsen, D. F. Callen, D. Sejer Pedersen, S. Nguyen, M. J. Sykes, O. Zvarec, A. D. Abell, Chem. Eur. J. 19: 7975-7981 (2013).

Petersen JG, Bergmann R, Møller HA, Jørgensen CG, Nielsen B, Kehler J, Frydenvang K, Kristensen J, Balle T, Jensen AA, Kristiansen U, Frølund B. Synthesis and Biological Evaluation of 4-(Aminomethyl)-1-hydroxypyrazole Analogues of Muscimol as γ-Aminobutyric AcidA Receptor Agonists. J. Med. Chem. 56: 993-1006 (2013).

Petersen, I.N., J.L. Kristensen, C. Tortzen, T. Breindahl and D. Sejer Pedersen. Synthesis and Stability Study of a New Major Metabolite of γ-Hydroxybutyric Acid. Beilstein J. Org. Chem. 9: 641-646 (2013).

Petersen, I.N., J.L. Kristensen, C. Tortzen, D. Sejer Pedersen, and T. Breindahl. Identification of a New Metabolite of GHB: Gamma-Hydroxybutyric Acid Glucuronide. J. Anal. Toxicol. 37: 291-7 (2013).

Reverte I, Klein AB, Domingo JL and Colomina MT. Long term effects of murine postnatal exposure to decabromodiphenyl ether (BDE-209) on learning and memory are dependent upon APOE polymorphism and age. Neurotoxicol. Teratol. 40: 17-27 (2013).

Rydberg, P., M. Rostkowski, D.E. Gloriam and L. Olsen. The contribution of atom accessibility to site of metabolism models for cytochromes P450. Mol. Pharm. 10: 1216-1223 (2013).

Quinn, S.J., A.R.B. Thomsen, J. Pang, L. Kantham, H. Bräuner-Osborne, M. Pollak D. Goltzman and E.M. Brown. Interactions between calcium and phosphorus in the regulation of the production of fibroblast growth factor 23 in vivo. Am. J. Physiol. Endocrinolol. Metab. 304: E310-E320 (2013).

Santini MA, Ratner C, Aznar S, Klein AB, Knudsen GM and Mikkelsen JD. Enhanced prefrontal serotonin 2A receptor signaling in the subchronic phencyclidine mouse model of schizophrenia. J. Neurosci. Res. 91: 634-641 (2013).

Smajilovic, S., C. Clemmensen, L.D. Johansen, P. Wellendorph, J.J. Holst, P.G. Thams, E. Ogo and H. Bräuner-Osborne. The L-α-amino acid receptor GPRC6A is expressed in the islets of Langerhans but is not involved in L-arginine induced insulin release. Amino Acids 44:383-390 (2013).

Ussing CA, Hansen CP, Petersen JG, Jensen AA, Rohde LA, Ahring PK, Nielsen EØ, Kastrup JS, Gajhede M, Frølund B, Balle T. Synthesis, Pharmacology, and Biostructural Characterization of Novel α4β2 Nicotinic Acetylcholine Receptor Agonists. J. Med. Chem. 56: 940-951 (2013).

Vogensen SB, Jørgensen L, Madsen KK, Borkar N, Wellendorph P, Skovgaard-Petersen J, Schousboe A, White HS, Krogsgaard-Larsen P, Clausen RP. Selective mGAT2 (BGT-1) GABA uptake inhibitors: Design, synthesis, and pharmacological characterization. J. Med. Chem. 56: 2160-4 (2013).

Vogensen SB, Marek A, Bay T, Wellendorph P, Kehler J, Bundgaard C, Frølund B, Pedersen MH, Clausen RP. New Synthesis and Tritium Labeling of a Selective Ligand for Studying High-Affinity γ-Hydroxybutyrate (GHB) Binding Sites. J. Med. Chem. 56: 8201-8205 (2013).

2012

Trattnig SM, Harpsøe K, Thygesen SB, Rahr LM, Ahring PK, Balle T, Jensen AA. Discovery of a novel allosteric modulator of 5-HT3 receptors: inhibition and potentiation of Cys-loop receptor signaling through a conserved transmembrane intersubunit site. J. Biol. Chem. 287: 25241-25254 (2012).

Huynh TH, Abrahamsen B, Madsen KK, Gonzalez-Franquesa A, Jensen AA, Bunch L. Design, synthesis and pharmacological characterization of coumarin-based fluorescent analogs of excitatory amino acid transporter subtype 1 selective inhibitors, UCPH-101 and UCPH-102. Bioorg. Med. Chem. 20: 6831-6839 (2012).

Rossol, M., Pierer, M., Quandt, D., Raulien, N., Meusch, U., Rothe, K., Schubert, K., Schöneberg, T., Schaefer, M., Krügel, U., Smajilovic, S., Bräuner-Osborne, H., Baerwald, C., Wagner, U. Extracellular Ca2+ is a danger signal activating the NLRP3 inflammasome through G protein-coupled calcium sensing receptors. Nature Commun. 3: 1329 (2012).

Thomsen, A.B.R., J. Worm, S.E. Jacobsen, M. Stahlhut, M. Latta and H. Bräuner-Osborne. Strontium is a biased agonist on the calcium-sensing receptor in rat medullary thyroid carcinoma 6-23 cells. J. Pharmacol. Exp. Ther. 343: 638-649 (2012).

Mølck, C., K. Harpsøe, D.E. Gloriam, R.P. Clausen, U. Madsen, L.Ø. Pedersen, H.N. Jimenez, S.M. Nielsen, J.M. Mathiesen and H. Bräuner-Osborne. Pharmacological characterization and modeling of the binding site of novel 1,3-bis(pyridinylethynyl)benzenes as metabotropic glutamate receptor 5-selective negative allosteric modulators. Mol. Pharmacol. 82: 929-937 (2012).

Thiele S, Malmgaard-Clausen M, Engel-Andreasen J, Steen A, Rummel PC, Nielsen MC, Gloriam DE, Frimurer TM, Ulven T, Rosenkilde MM. Modulation in selectivity and allosteric properties of small-molecule ligands for CC-chemokine receptors. J. Med. Chem. 55: 8164-77 (2012).

Soares da Costa TP, W. Tieu, N.R. Pendini, M.Y. Yap, S.W. Polyak, D. Sejer Pedersen, R. Morona, J.D. Turnige, J.C. Wallace, M.C.J. Wilce, G.W. Booker, A.D. Abell. Selective inhibition of biotin protein ligase from Staphylococcus Aureus. J. Biol. Chem. 287: 17823-17832 (2012).

Johansson H., and D. Sejer Pedersen. Azide- and alkyne-derivatised α-amino acids. Eur. J. Org. Chem. 23: 4267-4281 (2012).

Hedegaard, M.K., K.B. Hansen, K.T. Andersen, H. Bräuner-Osborne and S.F. Traynelis. Molecular pharmacology of human NMDA receptors. Neurochem. Int. 61: 601-609 (2012).

Absalom, N., L.F. Eghorn, I.S. Villumsen, N. Karim, T. Bay, J.V. Olsen, G.M. Knudsen, H. Bräuner-Osborne, B. Frølund, R.P. Clausen, M. Chebib and P. Wellendorph. α4βδ GABAA receptors are high-affinity targets for γ-hydroxybutyric acid (GHB). Proc. Natl. Acad. Sci. USA. 109: 13404-13409 (2012).

Thomsen, A.B.R., S. Smajilovic and H. Bräuner-Osborne. Novel strategies in drug discovery of the calcium-sensing receptor based on biased agonism. Curr. Drug Targets 13: 1324-1335 (2012).

Clemmensen, C., A.N. Madsen, S. Smajilovic, B. Holst and H. Bräuner-Osborne. L-Arginine improves multiple physiological parameters in mice exposed to diet-induced metabolic disturbances. Amino Acids 43: 1265-1275 (2012).

Huynh THV, Shim I, Bohr H, Abrahamsen B, Nielsen B, Jensen AA, Bunch L. Structure-activity relationship study of selective excitatory amino acid transporter subtype 1 (EAAT1) inhibitor 2-amino-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile (UCPH-101) and absolute configurational assignment using infrared and vibrational circular dichroism spectroscopy in combination with ab initio Hartree-Fock calculations. J Med Chem. 2012, 55:5403-5412.

Kaae BH, Harpsøe K, Kvist T, Mathiesen JM, Mølck C, Gloriam DE, Jimenez HN, Uberti MA, Nielsen SM, Nielsen B, Bräuner-Osborne H, Sauerberg P, Clausen RP, Madsen U. Structure-activity relationships for negative allosteric mGluR5 modulators. ChemMedChem. 2012, 7:440-451.

Karim N, Wellendorph P, Absalom N, Bang LH, Jensen ML, Hansen MM, Lee HJ, Johnston GAR, Hanrahan JR, Chebib M. Low nanomolar GABA effects at extrasynaptic α4β1/β3δ GABAA receptor subtypes indicate a different binding mode for GABA at these receptors. Biochem Pharmacol. 2012, 84:549-557.

Manglik A, Kruse AC, Kobilka TS, Thian FS, Mathiesen JM, Sunahara RK, Pardo L, Weis WI, Kobilka BK, Granie S. Crystal structure of the µ-opioid receptor bound to a morphinan antagonist. Nature. 2012, 485: 321–326.

Pan Y, Gerasimov MR, Kvist T, Wellendorph P, Madsen KK, Pera E, Lee H, Schousboe A, Chebib M, Bräuner-Osborne H, Craft CM, Brodie JD, Schiffer WK, Dewey SL, Miller SR, Silverman RB. (1S, 3S)-3-amino-4-difluoromethylenyl-1-cyclopentanoic acid (CPP-115), a potent γ-aminobutyric acid aminotransferase inactivator for the treatment of cocaine addiction. J Med Chem. 2012, 55:357-366.

Thomsen ARB, Hvidtfeldt M, Bräuner-Osborne H. Biased agonism of the calcium-sensing receptor. Cell Calcium. 2012, 51:107-116.

Zvarec O, Polyak SW, Tieu W, Kuan K, Dai H, Pedersen DS, Morona R, Zhang L, Booker GW, Abell AD. 5-benzylidenerhodanine and 5-benzylidene-2-4-thiazolidinedione based antibacterials. Bioorg Med Chem Lett. 2012, 22: 2720-2722.

2011

Armishaw CJ, Jensen AA, Balle LD, Scott KCM, Sørensen L, Strømgaard K. Improving the stability of α-conotoxin AuIB through N-to-C cyclization: The effect of linker length on stability and activity at nicotinic acetylcholine receptors. Antioxid Redox Signal. 2011, 14:65-76.

Davies MN, Gloriam DE, Flower DR. In silico identification of novel G protein-coupled receptors. I: Stevens CW, ed. Methods for the discovery and characterization of G protein-coupled receptors. New York: Humana Press. 2011, p. 3-18. (Neuromethods).

Davies MN, Gloriam DE, Secker A, Freitas AA, Timmis J, Flower DR. Present perspectives on the automated classification of the G-protein coupled receptors (GPCRs) at the protein sequence level. Curr Top Med Chem. 2011, 11:1994-2009.

Eljaja L, Bjerrum OJ, Honoré PGH, Abrahamsen B. Effects of the excitatory amino acid transporter subtype 2(EAAT-2) inducer ceftriaxone on different pain modalities in rat. Scand J Pain. 2011, 2:132-136.

Garland SL, Gloriam DE. A ligand's view of target similarity: chemogenomic binding site-directed techniques for drug discovery. Curr Top Med Chem. 2011, 11:1872-1881.

Gloriam DE, Wellendorph P, Johansen LD, Thomsen ARB, Phonekeo K, Pedersen DS, Bräuner-Osborne H. Chemogenomic discovery of allosteric antagonists at the GPRC6A receptor. Chem Biol. 2011, 18:1489-1498.

Heng S, Tieu W, Hautmann S, Kuan K, Pedersen DS, Pietsch M, Gütschow M, Abell AD. New cholesterol esterase inhibitors based on rhodanine and thiazolidinedione scaffolds. Bioorg Med Chem. 2011, 19:7453-7463.

Ísberg V, Balle T, Sander T, Jørgensen FS, Gloriam DEI. G protein- and agonist-bound serotonin 5-HT2A receptor model activated by steered molecular dynamics simulations. J Chem Inf Model. 2011, 51:315-325.

Jørgensen CG, Frølund BF, Kehler J, Jensen AA. Discovery of benzamide analogues as a novel class of 5-HT3 receptor agonists. ChemMedChem. 2011, 6:725-736.

Karim N, Gavande N, Wellendorph P, Johnston GAR, Hanrahan JR, Chebib M. 3-Hydroxy-2'-methoxy-6-methylflavone: A potent anxiolytic with a unique selectivity profile at GABAA receptor subtypes. Biochem Pharmacol. 2011, 82:1971-1983.

Kvist T, Hansen KB, Bräuner-Osborne H. The use of Xenopus oocytes in drug screening. Expert Opin Drug Discov. 2011, 6:141-153.

Nielsen SD, Fulco M, Serpi M, Nielsen B, Hansen MB, Hansen KL, Thomsen C, Brodbeck R, Bräuner-Osborne H, Pellicciari R, Norrby P, Greenwood JR, Clausen RP. A highly selective agonist for the metabotropic glutamate receptor mGluR2. MedChemComm. 2011, 2:1120-1124.

Pedersen DS, Abell A. 1,2,3-triazoles in peptidomimetic chemistry. Eur J Org Chem. 2011, 2011:2399-2411.

Rasmussen SGF, DeVree BT, Zou Y, Kruse AC, Chung KY, Kobilka TS, Thian FS, Chae PS, Pardon E, Calinski D, Mathiesen JM, Shah STA, Lyons JA, Caffrey M, Gellman SH, Steyaert J, Skiniotis G, Weis WI, Sunahara RK, Kobilka BK. Crystal structure of the β2 adrenergic receptor-Gs protein complex. Nature. 2011, 477:549-555.

Smajilovic S, Yano S, Jabbari R, Tfelt-Hansen J. The calcium-sensing receptor and calcimimetics in blood pressure modulation. Br J Pharmacol. 2011, 164:884-893.

Underwood CR, Knudsen SM, Wulff BS, Bräuner-Osborne H, Lau J, Knudsen LB, Peters GH, Reedtz-Runge S. Transmembrane α-helix 2 and 7 are important for small molecule-mediated activation of the GLP-1 receptor. Pharmacology. 2011, 88:340-348.

2010

Armishaw CJ, Singh N, Medina-Franco JL, Clark RJ, Scott KCM, Houghten RA, Jensen AA. A synthetic combinatorial strategy for developing α-conotoxin analogs as potent α7 nicotinic acetylcholine receptor antagonists. J Biol Chem. 2010, 285:1809-1821.

Conti P, Pinto A, Tamborini L, Madsen U, Nielsen B, Bräuner-Osborne H, Hansen KB, Landucci E, Pellegrini-Giampietro DE, De Sarro G, Donato Di Paola E, De Micheli C. Novel 3-carboxy- and 3-phosphonopyrazoline amino acids as potent and selective NMDA receptor antagonists: Design, synthesis, and pharmacological characterization. ChemMedChem. 2010, 5:1465-1475.

Erichsen MN, Huynh THV, Abrahamsen B, Bastlund JF, Bundgaard C, Monrad O, Bekker-Jensen A, Nielsen CW, Frydenvang KA, Jensen AA, Bunch L. Structure-activity relationship study of first selective inhibitor of excitatory amino acid transporter subtype 1: 2-amino-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile (UCPH-101). J Med Chem. 2010, 53:7180–7191.

Gloriam DEI, Orchard S, Bertinetti D, Björling E, Bongcam-Rudloff E, Borrebaeck CAK, Bourbeillon J, Bradbury ARM, de Daruvar A, Dübel S, Frank R, Gibson TJ, Gold L, Haslam N, Herberg FW, Hiltke T, Hoheisel JD, Kerrien S, Koegl M, Konthur Z, Korn B, Landegren U, Montecchi-Palazzi L, Palcy S, Rodriguez H, Schweinsberg S, Sievert V, Stoevesandt O, Taussig MJ, Ueffing M, Uhlén M, van der Maarel S, Wingren C, Woollard P, Sherman DJ, Hermjakob H. A community standard format for the representation of protein affinity reagents. Mol Cell Proteomics. 2010, 9:1-10.

Hansen KB, Mullasseril P, Dawit S, Kurtkaya NL, Yuan H, Vance KM, Orr AG, Kvist T, Ogden KK, Le P, Vellano KM, Lewis I, Kurtkaya S, Du Y, Qui M, Murphy TJ, Snyder JP, Bräuner-Osborne H, Traynelis SF. Implementation of a fluorescence-based screening assay identifies histamine H3 receptor antagonists clobenpropit and iodophenpropit as subunit-selective N-methyl-D-aspartate receptor antagonists. J Pharmacol Exp Ther. 2010, 333:650-662.

Jensen AA, Bergmann ML, Sander T, Balle T. Ginkgolide X is a potent antagonist of anionic Cys-loop receptors with a unique selectivity profile at glycine receptors. J Biol Chem. 2010, 285:10141-10153.

Krogsgaard-Larsen N, Jensen AA, Kehler J. Novel 7-phenylsulfanyl-1,2,3,4,10,10a-hexahydro-pyrazino[1,2-a]indoles as dual serotonin 5-HT2C and 5-HT6 receptor ligands. Bioorg Med Chem Lett. 2010, 20:5431-5433.

Mosley CA, Acker TM, Hansen KB, Mullasseril P, Andersen KT, Le P, Vellano KM, Bräuner-Osborne H, Liotta DC, Traynelis SF. Quinazolin-4-one derivatives: A novel class of noncompetitive NR2C/D subunit-selective N-methyl-D-aspartate receptor antagonists. J Med Chem. 2010, 53:5476-5490.

Møller HA, Sander T, Kristensen JL, Nielsen B, Krall J, Bergmann ML, Christiansen B, Balle T, Jensen AA, Frølund BF. Novel 4-(piperidin-4-yl)-1-hydroxypyrazoles as γ-aminobutyric acidA receptor ligands: synthesis, pharmacology, and structure-activity relationships. J Med Chem. 2010, 53:3417-3421.

Pedersen MHF, Høg S, Wellendorph P, Martiny L. Radioiododestannyllation of novel GHB neuroreceptor ligands. J Labelled Comp Radiopharm. 2010, 53:318-320.

Rydberg P, Gloriam DEI, Zaretzki J, Breneman C, Olsen L. SMARTCyp: A 2D method for prediction of cytochrome P450-mediated drug metabolism. ACS Med Chem Lett. 2010, 1:96-100.

Rydberg P, Gloriam DEI, Olsen L. The SMARTCyp cytochrome P450 metabolism prediction server. Bioinformatics. 2010, 26:2988-2989.

Sabbatini P, Wellendorph P, Høg S, Pedersen MHF, Bräuner-Osborne H, Martiny L, Frølund BF, Clausen RP. Design, synthesis, and in vitro pharmacology of new radiolabeled γ-hydroxybutyric acid analogues including photolabile analogues with irreversible binding to the high-affinity γ-hydroxybutyric acid binding sites. J Med Chem. 2010, 53:6506-6510.

Skovstrup S, Taboureau O, Bräuner-Osborne H, Jørgensen FS. Homology modelling of the GABA transporter and analysis of tiagabine binding. ChemMedChem. 2010, 5:986-1000.

Smajilovic S, Schaal-Jensen R, Jabbari R, Smajilovic U, Haunso S, Tfelt-Hansen J. Effect of intermittent versus continuous parathyroid hormone in the cardiovascular system of rats. Open Cardiovasc Med J. 2010, 4:110-116.

Stanley NJ, Pedersen DS, Nielsen B, Kvist T, Mathiesen JM, Bräuner-Osborne H, Taylor DK, Abell AD. 1,2,3-triazolyl amino acids as AMPA receptor ligands. Bioorg Med Chem Lett. 2010, 20:7512-7515.

Stanley NJ, Hutchinson MR, Kvist T, Nielsen B, Mathiesen JM, Bräuner-Osborne H, Avery TD, Tiekink ERT, Pedersen DS, Irvine RJ, Abell AD, Taylor DK. A new metabotropic glutamate receptor agonist with in vivo anti-allodynic activity. Bioorg Med Chem. 2010, 18:6089-6098.

Wellendorph P, Høg S, Sabbatini P, Pedersen MHF, Martiny L, Knudsen GM, Frølund BF, Clausen RP, Bräuner-Osborne H. Novel radioiodinated γ-hydroxybutyric acid analogues for radiolabeling and photolinking of high-affinity γ-hydroxybutyric acid binding sites. J Pharmacol Exp There. 2010, 335:458-464.

Wellendorph P, Johansen LD, Bräuner-Osborne H. The emerging role of promiscuous 7TM receptors as chemosensors for food intake. Vitamins & Hormones 84:151-184.

2009

Armishaw C, Jensen AA, Balle T, Clark RJ, Harpsøe K, Skonberg C, Liljefors T, Strømgaard K. Rational design of α-conotoxin analogues targeting α7 nicotinic acetylcholine receptors: Improved antagonistic activity by incorporation of proline derivatives. J Biol Chem. 2009, 284:9498-9512.

Bunch L, Pickering D, Gefflaut T, Vinatier V, Helaine V, Amir A, Nielsen B, Jensen AA. 4,4-Dimethyl- and diastereomeric 4-hydroxy-4-methyl-(2S)-glutamate analogues display distinct pharmacological profiles at ionotropic glutamate receptors and excitatory amino acid transporters. ChemMedChem. 2009, 4:1925-1929.

Bunch L, Erichsen MN, Jensen AA. Excitatory amino acid transporters as potential drug targets. Expert Opin Ther Targets. 2009, 13:719-731.

Clarke C, Foussat S, Fox DJ, Pedersen DS, Warren S. Asymmetric synthesis of trans-disubstituted cyclopropanes using phosphine oxides and phosphine boranes. Org Biomol Chem. 2009, 7:1323-1328.

Clarke C, Fox DJ, Pedersen DS, Warren S. The lithiation and acyl transfer reactions of phosphine oxides, sulfides and boranes in the synthesis of cyclopropanes. Org Biomol Chem. 2009, 7:1329-1336.

Clausen RP, Naur P, Kristensen AS, Greenwood JR, Strange M, Bräuner-Osborne H, Jensen AA, Nielsen AST, Geneser U, Ringgaard LM, Nielsen B, Pickering D, Brehm L, Gajhede M, Krogsgaard-Larsen P, Kastrup JS. The glutamate receptor GluR5 agonist (S)-2-amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic acid and the 8-methyl analogue: synthesis, molecular pharmacology, and biostructural characterization. J Med Chem. 2009, 52:4911-4922.

Faure H, Gorojankina T, Rice N, Dauban P, Dodd RH, Bräuner-Osborne H, Rognan D, Ruat M. Molecular determinants of non-competitive antagonist binding to the mouse GPRC6A receptor. Cell Calcium. 2009, 46:323-332.

Gloriam DEI, Foord SM, Blaney FE, Garland SL. Definition of the G protein-coupled receptor transmembrane bundle binding pocket and calculation of receptor similarities for drug design. J Med Chem. 2009, 52:4429-4442.

Guetg N, Seddik R, Vigot R, Turecek R, Gassmann M, Vogt KE, Bräuner-Osborne H, Shigemoto R, Kretz O, Frotscher M, Kulik Á, Bettler B. The GABAB1a isoform mediates heterosynaptic depression at hippocampal mossy fiber synapses. J Neurosci. 2009, 29:1414-1423.

Hansen CP, Jensen AA, Balle T, Bitsch-Jensen K, Hassan MM, Liljefors T, Frølund B. Carbamoylcholine analogs as nicotinic acetylcholine receptor agonists - structural modifications of 3-(dimethylamino)butyl dimethylcarbamate (DMABC). Bioorg Med Chem Lett. 2009, 19:87-91.

Hansen KB, Bräuner-Osborne H. FLIPR assays of intracellular calcium in GPCR drug discovery. Methods Mol Biol. 2009, 552:269-278.

Hansen KB, Bräuner-Osborne H. Xenopus oocyte electrophysiology in GPCR drug discovery. Methods Mol Biol. 2009, 552:343-357.

Jensen AA, Erichsen MN, Nielsen CW, Stensbøl TB, Kehler J, Bunch L. Discovery of the first selective inhibitor of excitatory amino acid transporter subtype 1. J Med Chem. 2009, 52:912-915.

Kvist T, Christiansen B, Jensen AA, Bräuner-Osborne H. The four human γ-aminobutyric acid (GABA) transporters: pharmacological characterization and validation of a highly efficient screening assay. Comb Chem High Throughput Screen. 2009, 12:241-249.

Lehmann A, Antonsson M, Holmberg AA, Blackshaw LA, Brändén L, Bräuner-Osborne H, Christiansen B, Dent J, Elebring T, Jacobson B, Jensen J, Mattsson JP, Nilsson K, Oja SS, Page AJ, Saransaari P, von Unge S. (R)-(3-amino-2-fluoropropyl) phosphinic acid (AZD3355), a novel GABAB receptor agonist, inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action. J Pharmacol Exp Ther. 2009, 331:504-512.

Pedersen DS, Robinson TV, Taylor DK, Tiekink ERT. A concise route to branched erythrono-γ-lactones. Synthesis of the leaf-closing substance potassium (+/-)-(2R,3R)-2,3,4-trihydroxy-2-methylbutanoate. J Org Chem. 2009, 74:4400-4403.

Wellendorph P, Bräuner-Osborne H. Molecular basis for amino acid sensing by family C G-protein-coupled receptors. Br J Pharmacol. 2009, 156:869-884.

Wellendorph P, Johansen LD, Bräuner-Osborne H. Molecular pharmacology of promiscuous seven transmembrane receptors sensing organic nutrients. Mol Pharmacol. 2009, 76(3):453-465.

Wellendorph P, Johansen LD, Jensen AA, Casanova E, Gassmann M, Deprez P, Clément-Lacroix P, Bettler B, Bräuner-Osborne H. No evidence for a bone phenotype in GPRC6A knockout mice under normal physiological conditions. J Mol Endocrinolol. 2009, 42:215-223.

Wellendorph P, Høg S, Skonberg C, Bräuner-Osborne H. Phenylacetic acids and the structurally related non-steroidal anti-inflammatory drug diclofenac bind to specific γ-hydroxybutyric acid sites in rat brain. Fundam Clin Pharmacol. 2009, 23:207-213.