Darryl S Pickering
Associate Professor
Molecular and Cellular Pharmacology
Jagtvej 160, København Ø
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(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 journal › Journal article › Research › peer-review
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(S)-2-Mercaptohistidine: A First Selective Orthosteric GluK3 Antagonist
Poulie, Christian Bernard Matthijs, Larsen, Y., Leteneur, C., Barthet, G., Bjørn-Yoshimoto, Walden, Malhaire, F., Nielsen, Birgitte, Pin, J. P., Mulle, C., Pickering, Darryl S & Bunch, Lennart, 2022, In: ACS Chemical Neuroscience. 13, 10, p. 1580–1587Research output: Contribution to journal › Journal article › Research › peer-review
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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. 6614-8Research output: Contribution to journal › Journal article › Research › peer-review
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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 journal › Journal article › Research › peer-review
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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 journal › Journal article › Research › peer-review
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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. 1925-1929Research output: Contribution to journal › Journal article › Research › peer-review
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4-Alkylated homoibotenic acid (HIBO) analogues: versatile pharmacological agents with diverse selectivity profiles towards metabotropic and ionotropic glutamate receptor subtypes
Madsen, Ulf, Pickering, Darryl S, Nielsen, Birgitte & Bräuner, Hans, 2005, In: Neuropharmacology. 49 Suppl 1, p. 114-9 5 p.Research output: Contribution to journal › Journal article › Research › peer-review
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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 journal › Journal article › Research › peer-review
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N-(7-(1H-imidazol-1-yl)-2,3-dioxo-6-(trifluoromethyl)-3,4-dihydroquinoxalin-1(2H)-yl)benzamide - a new kainate receptor selective antagonist and analgesic: Synthesis, X-ray crystallography, structure-affinity relationships, in vitro and in vivo pharmacology
Møllerud, S., Hansen, R. B., Pallesen, J. S., Temperini, Piero, Pasini, D., Bornholdt, J., Nielsen, Birgitte, Mamedova, Esmira, Chalupnik, P., Paternain, A. V., Lerma, J., Del Castillo, M. D., Andreasen T., Jesper, Frydenvang, Karla Andrea, Kastrup, Jette Sandholm Jensen, Johansen, Tommy Nørskov & Pickering, Darryl S, 2019, In: ACS Chemical Neuroscience. 10, p. 4685-4695 11 p.Research output: Contribution to journal › Journal article › Research › peer-review
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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, J. & Pickering, Darryl S, 20 Jan 2017, In: European Journal of Neuroscience. 45, 2, p. 238-248 11 p.Research output: Contribution to journal › Journal article › Research › peer-review
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A Diversity Oriented Synthesis Approach to New 2,3-trans-Substituted l-Proline Analogs as Potential Ligands for the Ionotropic Glutamate Receptors
Kayser, S., Temperini, Piero, Poulie, Christian Bernard Matthijs, Staudt, Markus, Nielsen, Birgitte, Pickering, Darryl S & Bunch, Lennart, 4 Mar 2020, In: ACS Chemical Neuroscience. 11, p. 702-714 13 p.Research output: Contribution to journal › Journal article › Research › peer-review
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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. 7289-7298Research output: Contribution to journal › Journal article › Research › peer-review
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A pharmacological profile of the high-affinity GluK5 kainate receptor
Møllerud, S., Kastrup, Jette Sandholm Jensen & Pickering, Darryl S, 2016, In: European Journal of Pharmacology. 788, p. 315-320 6 p.Research output: Contribution to journal › Journal article › Research › peer-review
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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. 206-213Research output: Contribution to journal › Journal article › Research › peer-review
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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. 2408-2414Research output: Contribution to journal › Journal article › Research › peer-review
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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 journal › Journal article › Research › peer-review
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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 journal › Journal article › Research › peer-review
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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 journal › Journal article › Research › peer-review
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Analogues of 3-Hydroxyisoxazole-Containing Glutamate Receptor Ligands Based on the 3-Hydroxypyrazole-Moiety: Design, Synthesis and Pharmacological Characterization
Jørgensen, L., Nielsen, Birgitte, Pickering, Darryl S, Kristensen, Anders Skov, Frydenvang, Karla Andrea, Madsen, Ulf & Clausen, Rasmus Prætorius, 2014, In: Neurochemical Research. 39, 10, p. 1895-1905 11 p.Research output: Contribution to journal › Journal article › Research › peer-review
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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 journal › Journal article › Research › peer-review
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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 journal › Journal article › Research › peer-review
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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 journal › Journal article › Research › peer-review
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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, L. & Pickering, Darryl S, 10 Feb 2017, In: Vascular Pharmacology. 90, p. 36-43 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
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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, R., Frydenvang, Karla Andrea, Gajhede, Michael, Bunch, Lennart, Pickering, Darryl S & Kastrup, Jette Sandholm Jensen, Dec 2011, In: Journal of Structural Biology. 176, 3, p. 307-314Research output: Contribution to journal › Journal article › Research › peer-review
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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. 8354-8361Research output: Contribution to journal › Journal article › Research › peer-review
ID: 1299533
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Investigation of the presence and antinociceptive function of muscarinic acetylcholine receptors in the African naked mole-rat (Heterocephalus glaber)
Research output: Contribution to journal › Journal article › Research › peer-review
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Discovery of the First Highly Selective Antagonist of the GluK3 Kainate Receptor Subtype
Research output: Contribution to journal › Journal article › Research › peer-review
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