Darryl S Pickering
Darryl S Pickering

Associate Professor


  1. Published

    (S)-2-Amino-3-(5-methyl-3-hydroxyisoxazol-4-yl)propanoic Acid (AMPA) and Kainate Receptor Ligands: Further Exploration of Bioisosteric Replacements, Structural and Biological Investigation.

    Brogi, S., Brindisi, M., Butini, S., Kshirsagar, G., Maramai, S., Chemi, G., Gemma, S., Campiani, G., Novellino, E., Fiorenzani, P., Pinassi, J., Aloisi, A. M., Gynther, M., Venskutonyte, R., Han, L., Frydenvang, Karla Andrea, Kastrup, Jette Sandholm Jensen & Pickering, Darryl S, 8 Mar 2018, In : Journal of Medicinal Chemistry. 61, 5, p. 2124-2130 7 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  2. Published

    1H-cyclopentapyrimidine-2,4(1H,3H)-dione-related ionotropic glutamate receptors ligands. Structure-activity relationships and identification of potent and selective iGluR5 modulators

    Butini, S., Pickering, Darryl S, Morelli, E., Coccone, S. S., Trotta, F., De Angelis, M., Guarino, E., Fiorini, I., Campiani, G., Novellino, E., Schousboe, Arne, Christensen, J. K. & Gemma, S., 2008, In : Journal of Medicinal Chemistry. 51, 20, p. 6614-8

    Research output: Contribution to journalJournal articleResearchpeer-review

  3. Published

    3-Substituted phenylalanines as selective AMPA- and kainate receptor ligands

    Szymanska, E., Pickering, Darryl S, Nielsen, Birgitte & Johansen, Tommy Nørskov, 2009, In : Bioorganic & Medicinal Chemistry. 17, 17, p. 6390-401 11 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  4. Published

    3-hydroxypyridazine 1-oxides as carboxylate bioisosteres: a new series of subtype-selective AMPA receptor agonists

    Greenwood, J. R., Mewett, K. N., Allan, R. D., Martín, B. O. & Pickering, Darryl S, Jul 2006, In : Neuropharmacology. 51, 1, p. 52-9 7 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  5. Published

    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

    Bunch, Lennart, Pickering, Darryl S, Gefflaut, T., Vinatier, V., Helaine, V., Amir, A., Nielsen, Birgitte & Jensen, Anders A., 2009, In : ChemMedChem. 4, 11, p. 1925-1929

    Research output: Contribution to journalJournal articleResearchpeer-review

  6. Published
  7. Published

    4-hydroxy-1,2,5-oxadiazol-3-yl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and molecular pharmacological characterization at ionotropic glutamate receptors of compounds related to glutamate and its homologues

    Lolli, M. L., Giordano, C., Pickering, Darryl S, Rolando, B., Hansen, K. B., Foti, A., Contreras-Sanz, A., Amir, A., Fruttero, R., Gasco, A., Nielsen, Birgitte & Johansen, Tommy Nørskov, 2010, In : Journal of Medicinal Chemistry. 53, 10, p. 4110-8 8 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  8. Published
  9. Published

    In vitro and in vivo effects of a novel dimeric inhibitor of PSD‐95 on excitotoxicity and functional recovery after experimental traumatic brain injury

    Sommer, J. B., Bach, Anders, Rytter, Hana Malá, Strømgaard, Kristian, Mogensen, Jesper & Pickering, Darryl S, 20 Jan 2017, In : European Journal of Neuroscience. 45, 2, p. 238-248 11 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  10. Published

    A new phenylalanine derivative acts as an antagonist at the AMPA receptor GluA2 and introduces partial domain closure: Synthesis, resolution, pharmacology, and crystal structure

    Szymanska, E., Frydenvang, Karla Andrea, Contreras-Sanz, A., Pickering, Darryl S, Frola, E., Serafimoska, Z., Nielsen, Birgitte, Kastrup, Jette Sandholm Jensen & Johansen, Tommy Nørskov, 4 Oct 2011, In : Journal of Medicinal Chemistry. 54, 20, p. 7289-7298

    Research output: Contribution to journalJournal articleResearchpeer-review

  11. Published

    A pharmacological profile of the high-affinity GluK5 kainate receptor

    Møllerud, Stine, Kastrup, Jette Sandholm Jensen & Pickering, Darryl S, 2016, In : European Journal of Pharmacology. 788, p. 315-320 6 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  12. Published

    A stereochemical anomaly: the cyclised (R)-AMPA analogue (R)-3-hydroxy-4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridine-5-carboxylic acid [(R)-5-HPCA] resembles (S)-AMPA at glutamate receptors

    Vogensen, S., Greenwood, J., Varming, A. R., Brehm, L., Pickering, Darryl S, Nielsen, Birgitte, Liljefors, T., Clausen, Rasmus Prætorius, Johansen, Tommy Nørskov & Krogsgaard-Larsen, Povl, 2004, In : Organic & Biomolecular Chemistry. 2, 2, p. 206-213

    Research output: Contribution to journalJournal articleResearchpeer-review

  13. Published

    A tetrazolyl-substituted subtype-selective AMPA receptor agonist

    Vogensen, S. B., Frydenvang, Karla Andrea, Greenwood, J. R., Postorino, G., Nielsen, Birgitte, Pickering, Darryl S, Ebert, B., Bølcho, U., Egebjerg, J., Gajhede, Michael, Kastrup, Jette Sandholm Jensen, Johansen, Tommy Nørskov, Clausen, Rasmus Prætorius & Krogsgaard-Larsen, Povl, 2007, In : Journal of Medicinal Chemistry. 50, 10, p. 2408-2414

    Research output: Contribution to journalJournal articleResearchpeer-review

  14. Published

    AMPA receptor mediated excitotoxicity in neocortical neurons is developmentally regulated and dependent upon receptor desensitization

    Jensen, J. B., Schousboe, Arne, Pickering, Darryl S & Pickering, Darryl S, 1998, In : Neurochemistry International. 32, 5-6, p. 505-13 8 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  15. Published

    Action of bicyclic isoxazole GABA analogues on GABA transporters and its relation to anticonvulsant activity

    Bolvig, T., Larsson, O. M., Pickering, Darryl S, Nelson, N., Falch, E., Krogsgaard-Larsen, Povl, Schousboe, Arne & Pickering, Darryl S, 1999, In : European Journal of Pharmacology. 375, 1-3, p. 367-74 7 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  16. Published

    Agonist discrimination between AMPA receptor subtypes

    Coquelle, T., Christensen, J. K., Banke, T. G., Madsen, U., Schousboe, Arne & Pickering, Darryl S, 2000, In : NeuroReport. 11, 12, p. 2643-8 5 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  17. Published
  18. Published

    Aryl- and heteroaryl-substituted phenylalanines as AMPA receptor ligands

    Szymańska, E., Chałupnik, P., Johansen, Tommy Nørskov, Nielsen, Birgitte, Cuñado Moral, A. M., Pickering, Darryl S & Kieć-Kononowicz, K., 1 Dec 2017, In : Chemical Biology & Drug Design. 90, p. 1271-1281 11 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  19. Published

    Augmentation of Anticancer Drug Efficacy in Murine Hepatocellular Carcinoma Cells by a Peripherally Acting Competitive N-Methyl-d-aspartate (NMDA) Receptor Antagonist

    Gynther, M., Proietti Silvestri, I., Hansen, J. C., Hansen, K. B., Malm, T., Ishchenko, Y., Larsen, Y., Han, L., Kayser, S., Auriola, S., Petsalo, A., Nielsen, Birgitte, Pickering, Darryl S & Bunch, Lennart, 14 Dec 2017, In : Journal of Medicinal Chemistry. 60, 23, p. 9885-9904 20 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  20. Published

    Binding Mode of an α-Amino Acid-Linked Quinoxaline-2,3-dione Analogue at Glutamate Receptor Subtype GluK1

    Demmer, C. S., Møller, C., Brown, P. M. G. E., Han, L., Pickering, Darryl S, Nielsen, Birgitte, Bowie, D., Frydenvang, Karla Andrea, Kastrup, Jette Sandholm Jensen & Bunch, Lennart, 9 Apr 2015, In : A C S Chemical Neuroscience. 6, p. 845-854 10 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  21. Published

    Binding and functional pharmacological characteristics of gepant-type antagonists in rat brain and mesenteric arteries

    Sheykhzade, Majid, Amandi, N., Pla, M. V., Abdolalizadeh, B., Sams, A., Warfvinge, K., Edvinsson, Lars & Pickering, Darryl S, 10 Feb 2017, In : Vascular Pharmacology. 90, p. 36-43 8 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  22. Published
  23. Published

    Biostructural and pharmacological studies of bicyclic analogues of the 3-isoxazolol glutamate receptor agonist ibotenic acid

    Frydenvang, Karla Andrea, Pickering, Darryl S, Greenwood, J. R., Krogsgaard-Larsen, N., Brehm, L., Nielsen, Birgitte, Vogensen, S. B., Hald, H., Kastrup, Jette Sandholm Jensen, Krogsgaard-Larsen, Povl & Clausen, Rasmus Prætorius, 10 Nov 2010, In : Journal of Medicinal Chemistry. 53, 23, p. 8354-8361

    Research output: Contribution to journalJournal articleResearchpeer-review

  24. Published

    Blood-brain barrier permeability and brain uptake mechanism of kainic Acid and dihydrokainic Acid

    Gynther, M., Petsalo, A., Hansen, S. H., Bunch, Lennart & Pickering, Darryl S, Mar 2015, In : Neurochemical Research. 40, 3, p. 542-549 8 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  25. Published

    Characterization of the 1H-cyclopentapyrimidine-2,4(1H,3H)-dione derivative (S)-CPW399 as a novel, potent, and subtype-selective AMPA receptor full agonist with partial desensitization properties

    Campiani, G., Morelli, E., Nacci, V., Fattorusso, C., Ramunno, A., Novellino, E., Greenwood, J., Liljefors, T., Griffiths, R., Sinclair, C., Reavy, H., Kristensen, A. S., Pickering, Darryl S, Schousboe, Arne, Cagnotto, A., Fumagalli, E., Mennini, T. & Pickering, Darryl S, 2001, In : Journal of Medicinal Chemistry. 44, 26, p. 4501-4 3 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  26. Published

    Chemo-enzymatic synthesis of (2S,4R)-2-amino-4-(3-(2,2-diphenylethylamino)-3-oxopropyl)pentanedioic acid: a novel selective inhibitor of human excitatory amino acid transporter subtype 2

    Sagot, E., Jensen, Anders A., Pickering, Darryl S, Pu, X., Umberti, M., Stensbøl, T. B., Nielsen, Birgitte, Assaf, Z., Aboab, B., Bolte, J., Gefflaut, T. & Bunch, Lennart, 2008, In : Journal of Medicinal Chemistry. 51, 14, p. 4085-4092 8 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  27. Published

    Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogues: new insight into the structure-activity relation of ionotropic glutamate receptor subtypes 5, 6, and 7.

    Sagot, E., Pickering, Darryl S, Pu, X., Umberti, M., Stensbøl, T. B., Nielsen, Birgitte, Chapelet, M., Bolte, J., Gefflaut, T. & Bunch, Lennart, 2008, In : Journal of Medicinal Chemistry. 51, 14, p. 4093-103

    Research output: Contribution to journalJournal articleResearchpeer-review

  28. Published

    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

    Assaf, Z., Larsen, A. P., Venskutonyte, R., Han, L., Abrahamsen, B., Nielsen, Birgitte, Gajhede, Michael, Kastrup, Jette Sandholm Jensen, Jensen, Anders A., Pickering, Darryl S, Frydenvang, Karla Andrea, Gefflaut, T. & Bunch, Lennart, 2013, In : Journal of Medicinal Chemistry. 56, 4, p. 1614-1628

    Research output: Contribution to journalJournal articleResearchpeer-review

  29. Published

    Cognitive enhancing effects of an AMPA receptor positive modulator on place learning in mice

    Rytter, Hana Malá, Chen, Y., Worm, V. H., Kure, J., Kaae, B. H., Madsen, Ulf, Badolo, L., Pickering, Darryl S & Mogensen, Jesper, 2012, In : Behavioural Brain Research. 226, 1, p. 18-25

    Research output: Contribution to journalJournal articleResearchpeer-review

  30. Published

    Computeren viser vejen til et nyt potentielt lægemiddel

    Harpsøe, Kasper, Kaae, B. H., Balle, T., Pickering, Darryl S & Kastrup, Jette Sandholm Jensen, 2008, In : Lægemiddelforskning. p. 28-30

    Research output: Contribution to journalJournal articleCommunication

  31. Published

    Convergent synthesis and pharmacology of substituted tetrazolyl-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid analogues

    Vogensen, S., Clausen, Rasmus Prætorius, Greenwood, J., Johansen, Tommy Nørskov, Pickering, Darryl S, Nielsen, Birgitte, Ebert, B. & Krogsgaard-Larsen, Povl, 5 May 2005, In : Journal of Medicinal Chemistry. 48, 9, p. 3438-3442

    Research output: Contribution to journalJournal articleResearchpeer-review

  32. Published

    Correlation between Anticonvulsant Activity and Inhibitory Action on Glial -Aminobutyric Acid Uptake of the Highly Selective Mouse -Aminobutyric Acid Transporter 1 Inhibitor 3-Hydroxy-4-amino-4,5,6,7-tetrahydro-1,2-benzisoxazole and Its N-Alkylated Analogs

    White, S., Sarup, A., Bolvig, T., Petersen, G., Nelson, N., Pickering, Darryl S, Larsson, O. M., Frølund, Bente, Falch, E., Krogsgaard-Larsen, Povl & Schousboe, Arne, 2002, In : Journal of Pharmacology and Experimental Therapeutics. 302, p. 636–644

    Research output: Contribution to journalJournal articleResearchpeer-review

  33. Published

    Crystal structure and pharmacological characterization of a novel N-methyl-D-aspartate (NMDA) receptor antagonist at the GluN1 glycine binding site

    Kvist, T., Steffensen, T. B., Greenwood, J. R., Mehrzad Tabrizi, F., Hansen, K. B., Gajhede, Michael, Pickering, Darryl S, Traynelis, S. F., Kastrup, Jette Sandholm Jensen & Bräuner-Osborne, Hans, 2013, In : The Journal of Biological Chemistry. 288, p. 33124-35 12 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  34. Published

    D-aspartate and NMDA, but not L-aspartate, block AMPA receptors in rat hippocampal neurons

    Gong, X., Frandsen, A., Lu, W., Wan, Y., Zabek, R. L., Pickering, Darryl S & Bai, D., 2005, In : British Journal of Pharmacology. 145, 4, p. 449-59 10 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  35. Published

    Depolarization-induced release of [(3)H]D-aspartate from GABAergic neurons caused by reversal of glutamate transporters

    Jensen, J. B., Pickering, Darryl S, Schousboe, Arne & Pickering, Darryl S, 2000, In : International Journal of Developmental Neuroscience. 18, 2-3, p. 309-15 6 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  36. Published

    Design and Synthesis of 2,3-trans-Proline Analogs as Ligands for the Ionotropic Glutamate Receptors and the Excitatory Amino Acid Transporters

    Poulie, Christian Bernard Matthijs, Alcaide Lopez, A., Krell-Jørgensen, M. P., Larsen, Y., Astier, E., Bjørn-Yoshimoto, Walden, Yi, F., Syrenne, J. T., Storgaard, M., Nielsen, Birgitte, Frydenvang, Karla Andrea, Jensen, Anders A., Hansen, K. B., Pickering, Darryl S & Bunch, Lennart, 19 Jun 2019, In : A C S Chemical Neuroscience. 10, 6, p. 2989-3007 19 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  37. Published

    Design and Synthesis of a Series of L-trans-4-Substituted Prolines as Selective Antagonists for the Ionotropic Glutamate Receptors Including Functional and X-ray Crystallographic Studies of New Subtype Selective Kainic Acid Receptor Subtype 1 (GluK1) Antagonist (2S,4R)-4-(2-Carboxyphenoxy)pyrrolidine-2-carboxylic Acid

    Krogsgaard-Larsen, N., Delgar, C., Koch, K., Brown, P. M. G. E., Møller, C., Han, L., Huynh, T. H. V., Hansen, S. W., Nielsen, Birgitte, Bowie, D., Pickering, Darryl S, Kastrup, Jette Sandholm Jensen, Frydenvang, Karla Andrea & Bunch, Lennart, 2017, In : Journal of Medicinal Chemistry. 60, 1, p. 441-457 17 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  38. Published

    Design and characterization of dimeric ligands cross-linking two identical modulatory AMPA receptor sites

    Kaae, B. H., Harpsøe, Kasper, Sanz, A. C., Pickering, Darryl S, Sauerberg, P., Clausen, Rasmus Prætorius, Kastrup, Jette Sandholm Jensen, Liljefors, T. & Madsen, Ulf, 19 Aug 2007, In : American Chemical Society. Abstracts of Papers (at the National Meeting). 234

    Research output: Contribution to journalConference abstract in journalResearch

  39. Published
  40. Published

    Design, synthesis and structure-activity relationships of novel phenylalanine-based amino acids as kainate receptors ligands

    Szymańska, E., Chałupnik, P., Szczepańska, K., Moral, A. M. C., Pickering, Darryl S, Nielsen, Birgitte, Johansen, Tommy Nørskov & Kieć-Kononowicz, K., 2016, In : Bioorganic & Medicinal Chemistry Letters. 26, 22, p. 5568-5572 5 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  41. Published

    Design, synthesis, and pharmacology of a highly subtype-selective GluR1/2 agonist, (RS)-2-amino-3-(4-chloro-3-hydroxy-5-isoxazolyl)propionic acid (Cl-HIBO)

    Bjerrum, E. J., Kristensen, Anders Skov, Pickering, D. S., Greenwood, J. R., Nielsen, Birgitte, Liljefors, T., Schousboe, Arne, Bräuner-Osborne, Hans, Madsen, Ulf & Pickering, Darryl S, 2003, In : Journal of Medicinal Chemistry. 46, 11, p. 2246-9 3 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  42. Published

    Development of calcium-permeable alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors in cultured neocortical neurons visualized by cobalt staining

    Jensen, J. B., Schousboe, Arne, Pickering, Darryl S & Pickering, Darryl S, 1998, In : Journal of Neuroscience Research. 54, 2, p. 273-81 8 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  43. Published

    Differential role of AMPA receptors in mouse tests of antidepressant and anxiolytic action

    Andreasen T., Jesper, Fitzpatrick, C. M., Larsen, M., Skovgaard, L., Nielsen, S. D., Clausen, Rasmus Prætorius, Troelsen, K. & Pickering, Darryl S, 19 Mar 2015, In : Brain Research. 1601, p. 117-26 10 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  44. Published

    Discovery of a New Class of Ionotropic Glutamate Receptor Antagonists by the Rational Design of (2S,3R)-3-(3-Carboxyphenyl)-pyrrolidine-2-carboxylic Acid

    Larsen, A. M., Venskutonyte, R., Valadés, E. A., Nielsen, Birgitte, Pickering, Darryl S & Bunch, Lennart, 4 Nov 2011, In : ACS Chemical Neuroscience. 2, 2, p. 107-114 8 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  45. Published

    Does increasing the ratio of AMPA-to-NMDA receptor mediated neurotransmission engender antidepressant action? Studies in the mouse forced swim and tail suspension tests

    Andreasen T., Jesper, Gynther, M. O. O., Rygaard, A., Bøgelund, T., Nielsen, S. D., Clausen, Rasmus Prætorius, Mogensen, Jesper & Pickering, Darryl S, 2013, In : Neuroscience Letters. 546, p. 6-10 4 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  46. Published

    Effect of synthetic and natural phospholipids on N-acylphosphatidylethanolamine-hydrolyzing phospholipase D activity

    Petersen, G., Pedersen, A. H., Pickering, Darryl S, Begtrup, M. & Hansen, Harald S., 2009, In : Chemistry and Physics of Lipids. 162, 1-2, p. 53-61

    Research output: Contribution to journalJournal articleResearchpeer-review

  47. Published

    Effects of dimeric PSD-95 inhibition on excitotoxic cell death and outcome after controlled cortical impact in rats: PSD-95 inhibition in experimental TBI

    Sommer, J. B., Bach, Anders, Rytter, Hana Malá, Gynther, M., Bjerre, A., Gram, M. G., Marschner, L., Strømgaard, Kristian, Mogensen, Jesper & Pickering, Darryl S, 2017, In : Neurochemical Research. 42, 12, p. 3401-3413 13 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  48. Published

    Effects of sertraline, duloxetine, vortioxetine, and idazoxan in the rat affective bias test

    Refsgaard, L. K., Haubro, K., Pickering, Darryl S, Stuart, S., Robinson, E. & Andreasen T., Jesper, 14 Oct 2016, In : Psychopharmacology. 233, 21, p. 3763-3770 8 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  49. Published

    Effects of the dimeric PSD-95 inhibitor UCCB01-144 in mouse models of pain, cognition and motor function

    Andreasen T., Jesper, Nasser, A., Caballero Puntiverio, Maitane, Sahlholt, M., Bach, Anders, Gynther, M., Strømgaard, Kristian & Pickering, Darryl S, 5 Jun 2016, In : European Journal of Pharmacology. 780, p. 166-73 8 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

  50. Published

    Effects of the dimeric PSD-95 inhibitor UCCB01-144 on functional recovery after fimbria-fornix transection in rats

    Sommer, J. B., Bach, Anders, Rytter, Hana Malá, Strømgaard, Kristian, Mogensen, Jesper & Pickering, Darryl S, Oct 2017, In : Pharmacology, Biochemistry and Behavior. 161, p. 62-67 6 p.

    Research output: Contribution to journalJournal articleResearchpeer-review

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