Synthesis and pharmacology of 3-isoxazolol amino acids as selective antagonists at group I metabotropic glutamic acid receptors

…, F Bischoff, P Krogsgaard-Larsen

Index: Madsen; Braeuner-Osborne; Frydenvang; Hvene; Johansen; Nielsen; Sanchez; Stensbol; Bischoff; Krogsgaard-Larsen Journal of Medicinal Chemistry, 2001 , vol. 44, # 7 p. 1051 - 1059

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Citation Number: 22

Abstract

Using ibotenic acid (2) as a lead, two series of 3-isoxazolol amino acid ligands for (S)- glutamic acid (Glu, 1) receptors have been developed. Whereas analogues of (RS)-2-amino- 3-(3-hydroxy-5-methyl-4-isoxazolyl) propionic acid [AMPA,(RS)-3] interact selectively with ionotropic Glu receptors (iGluRs), the few analogues of (RS)-2-amino-3-(3-hydroxy-5- isoxazolyl) propionic acid [HIBO,(RS)-4] so far known typically interact with iGluRs as well ...