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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 and Structural and Biological Investigation.
Brogi S, Brindisi M, Butini S, Kshirsagar GU, Maramai S, Chemi G, Gemma S, Campiani G, Novellino E, Fiorenzani P, Pinassi J, Aloisi AM, Gynther M, Venskutonytė R, Han L, Frydenvang K, Kastrup JS, Pickering DS. Brogi S, et al. Among authors: pickering ds. J Med Chem. 2018 Mar 8;61(5):2124-2130. doi: 10.1021/acs.jmedchem.8b00099. Epub 2018 Feb 26. J Med Chem. 2018. PMID: 29451794
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 AS, Pickering DS, Schousboe A, Cagnotto A, Fumagalli E, Mennini T. Campiani G, et al. Among authors: pickering ds. J Med Chem. 2001 Dec 20;44(26):4501-4. doi: 10.1021/jm015552m. J Med Chem. 2001. PMID: 11741469
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 AR, Brehm L, Pickering DS, Nielsen B, Liljefors T, Clausen RP, Johansen TN, Krogsgaard-Larsen P. Vogensen SB, et al. Among authors: pickering ds. Org Biomol Chem. 2004 Jan 21;2(2):206-13. doi: 10.1039/b310450h. Epub 2003 Nov 24. Org Biomol Chem. 2004. PMID: 14737644
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: pickering ds. J Med Chem. 2007 May 17;50(10):2408-14. doi: 10.1021/jm061439q. Epub 2007 Apr 25. J Med Chem. 2007. PMID: 17455929
126 results