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Synthesis and Pharmacology of Mono-, Di-, and Trialkyl-Substituted 7-Chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-Dioxides Combined with X-ray Structure Analysis to Understand the Unexpected Structure-Activity Relationship at AMPA Receptors.
Larsen AP, Francotte P, Frydenvang K, Tapken D, Goffin E, Fraikin P, Caignard DH, Lestage P, Danober L, Pirotte B, Kastrup JS. Larsen AP, et al. Among authors: kastrup js. ACS Chem Neurosci. 2016 Mar 16;7(3):378-90. doi: 10.1021/acschemneuro.5b00318. Epub 2016 Feb 1. ACS Chem Neurosci. 2016. PMID: 26771108
A tetrazolyl-substituted subtype-selective AMPA receptor agonist.
Vogensen SB, Frydenvang K, Greenwood JR, Postorino G, Nielsen B, Pickering DS, Ebert B, Bølcho U, Egebjerg J, Gajhede M, Kastrup JS, Johansen TN, Clausen RP, Krogsgaard-Larsen P. Vogensen SB, et al. Among authors: kastrup js. J Med Chem. 2007 May 17;50(10):2408-14. doi: 10.1021/jm061439q. Epub 2007 Apr 25. J Med Chem. 2007. PMID: 17455929
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 DS, Mirza O, Johansen TN, Greenwood J, Vestergaard B, Schousboe A, Gajhede M, Liljefors T, Kastrup JS. Beich-Frandsen M, et al. Among authors: kastrup js. J Med Chem. 2008 Mar 13;51(5):1459-63. doi: 10.1021/jm701126w. Epub 2008 Feb 13. J Med Chem. 2008. PMID: 18269227
Full domain closure of the ligand-binding core of the ionotropic glutamate receptor iGluR5 induced by the high affinity agonist dysiherbaine and the functional antagonist 8,9-dideoxyneodysiherbaine.
Frydenvang K, Lash LL, Naur P, Postila PA, Pickering DS, Smith CM, Gajhede M, Sasaki M, Sakai R, Pentikaïnen OT, Swanson GT, Kastrup JS. Frydenvang K, et al. Among authors: kastrup js. J Biol Chem. 2009 May 22;284(21):14219-29. doi: 10.1074/jbc.M808547200. Epub 2009 Mar 18. J Biol Chem. 2009. PMID: 19297335 Free PMC article.
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 RP, Naur P, Kristensen AS, Greenwood JR, Strange M, Bräuner-Osborne H, Jensen AA, Nielsen AS, Geneser U, Ringgaard LM, Nielsen B, Pickering DS, Brehm L, Gajhede M, Krogsgaard-Larsen P, Kastrup JS. Clausen RP, et al. Among authors: kastrup js. J Med Chem. 2009 Aug 13;52(15):4911-22. doi: 10.1021/jm900565c. J Med Chem. 2009. PMID: 19588945
150 results