Darryl S Pickering
Associate Professor
Molecular and Cellular Pharmacology
Jagtvej 160, København Ø
- Published
Synthesis and Pharmacological Characterization of the Selective GluK1 Radioligand (S)-2-Amino-3-(6-[3H]-2,4-dioxo-3,4-dihydrothieno[3,2-d]pyrimidin-1(2H)-yl)propanoic acid ([3H]-NF608)
Alcaide, A., Marconi, L., Marek, A., Haym, I., Nielsen, Birgitte, Møllerud, S., Jensen, M., Conti, P., Pickering, Darryl S & Bunch, Lennart, 2016, In: MedChemComm. 7, p. 2136-2144 9 p.Research output: Contribution to journal › Journal article › Research › peer-review
- 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 journal › Journal article › Research › peer-review
- 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, M., 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 journal › Journal article › Research › peer-review
- Published
UCCB01-125, a dimeric inhibitor of PSD-95, reduces inflammatory pain without disrupting cognitive or motor performance: Comparison with the NMDA receptor antagonist MK-801
Andreasen T., Jesper, Bach, Anders, Gynther, M., Nasser, A., Mogensen, J., Strømgaard, Kristian & Pickering, Darryl S, Apr 2013, In: Neuropharmacology. 67, p. 193-200 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
- 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, J. & Pickering, Darryl S, 2013, In: Neuroscience Letters. 546, p. 6-10 4 p.Research output: Contribution to journal › Journal article › Research › peer-review
- 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. 1614-1628Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Erratum: Chemoenzymatic synthesis of new 2,4- syn -functionalized (S)-glutamate analogues and structure-activity relationship studies at ionotropic glutamate receptors and excitatory amino acid transporters (Journal of Medicinal Chemistry (2013) 56 (1614-1628))
Assaf, Z., Larsen, A. P., Venskutonyteì, R., Han, L., Abrahamsen, B., Nielsen, Birgitte, Gajhede, Michael, Kastrup, Jette Sandholm Jensen, Jensen, A. A., Pickering, Darryl S, Frydenvang, Karla Andrea, Gefflaut, T. & Bunch, Lennart, 25 Jul 2013, In: Journal of Medicinal Chemistry. 56, 14, p. 5985 1 p.Research output: Contribution to journal › Comment/debate › Research › peer-review
- Published
Small-molecule positive allosteric modulation of homomeric kainate receptors GluK1-3: development of screening assays and insight into GluK3 structure
Bay, Yasmin, Venskutonytė, R., Frantsen, S. M., Thorsen, T. S., Musgaard, M., Frydenvang, Karla Andrea, Francotte, P., Pirotte, B., Biggin, P. C., Kristensen, Anders Skov, Boesen, T., Pickering, Darryl S, Gajhede, Michael & Kastrup, Jette Sandholm Jensen, 2024, In: FEBS Journal. 291, 7, p. 1506-1529Research output: Contribution to journal › Journal article › Research › peer-review
- Published
The positive allosteric modulator BPAM344 and L-glutamate introduce an active-like structure of the ligand-binding domain of GluK2
Bay, Yasmin, Egeberg Jeppesen, M., Frydenvang, Karla Andrea, Francotte, P., Pirotte, B., Pickering, Darryl S, Kristensen, Anders Skov & Kastrup, Jette Sandholm Jensen, 2024, In: FEBS Letters. 598, 7, p. 743-757Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Structures of the ligand-binding core of iGluR2 in complex with the agonists (R)- and (S)-2-amino-3-(4-hydroxy-1,2,5-thiadiazol-3-yl)propionic acid explain their unusual equipotency
Beich-Frandsen, M., Pickering, Darryl S, Mirza, Osman Asghar, Johansen, Tommy Nørskov, Greenwood, J., Vestergaard, Bente, Schousboe, Arne, Gajhede, Michael, Liljefors, T. & Kastrup, Jette Sandholm Jensen, 2008, In: Journal of Medicinal Chemistry. 51, 5, p. 1459-63Research output: Contribution to journal › Journal article › Research › peer-review
- 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, Hans, Madsen, Ulf & Pickering, Darryl S, 2003, In: Journal of Medicinal Chemistry. 46, 11, p. 2246-9 3 p.Research output: Contribution to journal › Journal article › Research › peer-review
- 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 journal › Journal article › Research › peer-review
- 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 journal › Journal article › Research › peer-review
- Published
Pharmacological characterization of (4R)-alkyl glutamate analogues at the ionotropic glutamate receptors: focus on subtypes iGlu5-7
Bunch, Lennart, Gefflaut, T., Alaux, S., Sagot, E., Nielsen, Birgitte & Pickering, Darryl S, 2009, In: European Journal of Pharmacology. 609, p. 1-4Research output: Contribution to journal › Journal article › Research › peer-review
- 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. 1925-1929Research output: Contribution to journal › Journal article › Research › peer-review
- 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. 6614-8Research output: Contribution to journal › Journal article › Research › peer-review
- 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 journal › Journal article › Research › peer-review
- Published
Structure-Activity Relationship and Solubility Studies of Novel N1-substituted Quinoxaline-2,3-diones as Kainate Receptor Antagonists
Chałupnik, P., Vialko, A., Pickering, Darryl S, Nielsen, B., Bay, Yasmin, Kristensen, Anders Skov, Hinkkanen, M., Szczepańska, K., Karcz, T., Latacz, G., Johansen, Tommy Nørskov & Szymanska, E. M., 2023, In: ChemMedChem. 18, 18, 15 p., e202300278.Research output: Contribution to journal › Journal article › Research › peer-review
- Accepted/In press
Tritium and deuterium labelling of a kainate receptor antagonist and evaluation as a radioligand
Chałupnik, P., Marek, A., Hovah, M. E. L., Pickering, Darryl S, Temperini, Piero, Donbosco, S., Szymańska, E. & Johansen, Tommy Nørskov, 2024, (Accepted/In press) In: Journal of Labelled Compounds and Radiopharmaceuticals.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Discovery of the First Highly Selective Antagonist of the GluK3 Kainate Receptor Subtype
Chałupnik, P., Vialko, A., Pickering, Darryl S, Hinkkanen, M., Donbosco, S., Møller, T. C., Jensen, Anders A., Nielsen, Birgitte, Bay, Yasmin, Kristensen, Anders Skov, Johansen, Tommy Nørskov, Łątka, K., Bajda, M. & Szymańska, E., 2022, In: International Journal of Molecular Sciences. 23, 15, 16 p., 8797.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
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
Clausen, Rasmus Prætorius, Naur, P., Kristensen, Anders Skov, Greenwood, J. R., Strange, M., Bräuner, Hans, Jensen, Anders A., Nielsen, A. S. T., Geneser, U., Ringgaard, L. M., Nielsen, Birgitte, Pickering, Darryl S, Brehm, L., Gajhede, Michael, Krogsgaard-Larsen, Povl & Kastrup, Jette Sandholm Jensen, 2009, In: Journal of Medicinal Chemistry. 52, 15, p. 4911-4922Research output: Contribution to journal › Journal article › Research › peer-review
- 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 journal › Journal article › Research › peer-review
- 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 journal › Journal article › Research › peer-review
- Published
Revisiting the Quinoxalinedione scaffold in the Construction of New Ligands for the Ionotropic Glutamate Receptors.
Demmer, C. S., Rombach, D., Liu, N., Nielsen, Birgitte, Pickering, Darryl S & Bunch, Lennart, 1 Dec 2017, In: A C S Chemical Neuroscience. 8, 11, p. 2477-2495 19 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Molecular determinants of desensitization and assembly of the chimeric GABA(A) receptor subunits (alpha1/gamma2) and (gamma2/alpha1) in combinations with beta2 and gamma2
Elster, L., Kristiansen, Uffe, Pickering, Darryl S, Olsen, R. W. & Schousboe, Arne, 2001, In: Neurochemistry International. 38, 7, p. 581-92 11 p.Research 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
Published