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, Simone; Brindisi, Marghertia; Butini, Stefania; Kshirsagar, Giridhar; Maramai, Samuele; Chemi, Giulia; Gemma, Sandra; Campiani, Giuseppe; Novellino, Ettore; Fiorenzani, Paolo; Pinassi, Jessica; Aloisi, Anna Maria; Gynther, Mikko; Venskutonyte, Raminta; Han, Liwei; Frydenvang, Karla Andrea; Kastrup, Jette Sandholm Jensen; Pickering, Darryl S.

    In: Journal of Medicinal Chemistry, Vol. 61, No. 5, 08.03.2018, p. 2124-2130.

    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, Stefania; Pickering, Darryl S; Morelli, Elena; Coccone, Salvatore Sanna; Trotta, Francesco; De Angelis, Meri; Guarino, Egeria; Fiorini, Isabella; Campiani, Giuseppe; Novellino, Ettore; Schousboe, Arne; Christensen, Jeppe K; Gemma, Sandra.

    In: Journal of Medicinal Chemistry, Vol. 51, No. 20, 2008, p. 6614-8.

    Research output: Contribution to journalJournal articleResearchpeer-review

  3. Published

    3-Substituted phenylalanines as selective AMPA- and kainate receptor ligands. / Szymanska, Ewa; Pickering, Darryl S; Nielsen, Birgitte; Johansen, Tommy N.

    In: Bioorganic & Medicinal Chemistry, Vol. 17, No. 17, 2009, p. 6390-401.

    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, Jeremy R; Mewett, Ken N; Allan, Robin D; Martín, Belén Ortiz; Pickering, Darryl.

    In: Neuropharmacology, Vol. 51, No. 1, 07.2006, p. 52-9.

    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, Thierry; Vinatier, Virginie; Helaine, Virgil; Amir, Ahmad; Nielsen, Birgitte; Jensen, Anders Asbjørn.

    In: ChemMedChem, Vol. 4, No. 11, 2009, 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, Marco L; Giordano, Cecilia; Pickering, Darryl S; Rolando, Barbara; Hansen, Kasper B; Foti, Antonio; Contreras-Sanz, Alberto; Amir, Ahmad; Fruttero, Roberta; Gasco, Alberto; Nielsen, Birgitte; Johansen, Tommy N.

    In: Journal of Medicinal Chemistry, Vol. 53, No. 10, 2010, p. 4110-8.

    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, Jens Bak; Bach, Anders; Rytter, Hana Malá; Strømgaard, Kristian; Mogensen, Jesper; Pickering, Darryl S.

    In: European Journal of Neuroscience, Vol. 45, No. 2, 20.01.2017, p. 238-248.

    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, Ewa; Frydenvang, Karla; Contreras-Sanz, Alberto; Pickering, Darryl S; Frola, Elena; Serafimoska, Zorica; Nielsen, Birgitte; Kastrup, Jette Sandholm; Johansen, Tommy Nørskov.

    In: Journal of Medicinal Chemistry, Vol. 54, No. 20, 04.10.2011, 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.

    In: European Journal of Pharmacology, Vol. 788, 2016, p. 315-320.

    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, SB; Greenwood, JR; Varming, Annemarie R.; Brehm, L; Pickering, DS; Nielsen, Birgitte; Liljefors, T; Clausen, Rasmus Prætorius; Johansen, Tommy Nørskov; Krogsgaard-Larsen, P.

    In: Organic & Biomolecular Chemistry, Vol. 2, No. 2, 2004, p. 206-213.

    Research output: Contribution to journalJournal articleResearchpeer-review

  13. Published

    A tetrazolyl-substituted subtype-selective AMPA receptor agonist. / Vogensen, Stine Byskov; Frydenvang, Karla Andrea; Greenwood, Jeremy R.; Postorino, Giovanna; Nielsen, Birgitte; Pickering, Darryl Scott; Ebert, Bjarke; Bølcho, Ulrik; Egebjerg, Jan; Gajhede, Michael; Kastrup, Jette Sandholm Jensen; Johansen, Tommy Nørskov; Clausen, Rasmus Prætorius; Krogsgaard-Larsen, Povl.

    In: Journal of Medicinal Chemistry, Vol. 50, No. 10, 2007, 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, A; Pickering, D S; Pickering, Darryl.

    In: Neurochemistry International, Vol. 32, No. 5-6, 1998, p. 505-13.

    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, D S; Nelson, N; Falch, E; Krogsgaard-Larsen, P; Schousboe, A; Pickering, Darryl.

    In: European Journal of Pharmacology, Vol. 375, No. 1-3, 1999, p. 367-74.

    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, A; Pickering, Darryl.

    In: NeuroReport, Vol. 11, No. 12, 2000, p. 2643-8.

    Research output: Contribution to journalJournal articleResearchpeer-review

  17. Published
  18. Published

    Aryl- and heteroaryl-substituted phenylalanines as AMPA receptor ligands. / Szymańska, Ewa; Chałupnik, Paulina; Johansen, Tommy Nørskov; Nielsen, Birgitte; Cuñado Moral, Ana Maria; Pickering, Darryl S; Kieć-Kononowicz, Katarzyna.

    In: Chemical Biology & Drug Design, Vol. 90, 01.12.2017, p. 1271-1281.

    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, Mikko; Proietti Silvestri, Ilaria; Hansen, Jacob C; Hansen, Kasper B; Malm, Tarja; Ishchenko, Yevheniia; Larsen, Younes; Han, Liwei; Kayser, Silke; Auriola, Seppo; Petsalo, Aleksanteri; Nielsen, Birgitte; Pickering, Darryl S; Bunch, Lennart.

    In: Journal of Medicinal Chemistry, Vol. 60, No. 23, 14.12.2017, p. 9885-9904.

    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, Charles S; Møller, Charlotte; Brown, Patricia M G E; Han, Liwei; Pickering, Darryl S; Nielsen, Birgitte; Bowie, Derek; Frydenvang, Karla; Kastrup, Jette S; Bunch, Lennart.

    In: A C S Chemical Neuroscience, Vol. 6, 09.04.2015, p. 845-854.

    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, Nilofar; Pla, Monica Vidal; Abdolalizadeh, Bahareh; Sams, Anette; Warfvinge, Karin; Edvinsson, Lars; Pickering, Darryl S.

    In: Vascular Pharmacology, Vol. 90, 10.02.2017, p. 36-43.

    Research output: Contribution to journalJournal articleResearchpeer-review

  22. Published

    Binding site and interlobe interactions of the ionotropic glutamate receptor GluK3 ligand binding domain revealed by high resolution crystal structure in complex with (S)-glutamate. / Venskutonyte, Raminta; Frydenvang, Karla; Gajhede, Michael; Bunch, Lennart; Pickering, Darryl S; Kastrup, Jette Sandholm.

    In: Journal of Structural Biology, Vol. 176, No. 3, 12.2011, p. 307-314.

    Research output: Contribution to journalJournal articleResearchpeer-review

  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, Jeremy R; Krogsgaard-Larsen, Niels; Brehm, Lotte; Nielsen, Birgitte; Vogensen, Stine Byskov; Hald, Helle; Kastrup, Jette Sandholm; Krogsgaard-Larsen, Povl; Clausen, Rasmus Prætorius.

    In: Journal of Medicinal Chemistry, Vol. 53, No. 23, 10.11.2010, 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, Mikko; Petsalo, Aleksanteri; Hansen, Steen Honoré; Bunch, Lennart; Pickering, Darryl S.

    In: Neurochemical Research, Vol. 40, No. 3, 03.2015, p. 542-549.

    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, D S; Schousboe, A; Cagnotto, A; Fumagalli, E; Mennini, T; Pickering, Darryl.

    In: Journal of Medicinal Chemistry, Vol. 44, No. 26, 2001, p. 4501-4.

    Research output: Contribution to journalJournal articleResearchpeer-review

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