(2<i>S</i>,1‘<i>S</i>,2‘<i>S</i>,3‘<i>R</i>)-2-(2‘-Carboxy-3‘-methylcyclopropyl) Glycine Is a Potent and Selective Metabotropic Group 2 Receptor Agonist with Anxiolytic Properties
作者:Iván Collado、Concepción Pedregal、Angel Mazón、Juan Félix Espinosa、Jaime Blanco-Urgoiti、Darryle D. Schoepp、Rebecca A. Wright、Bryan G. Johnson、Ann E. Kingston
DOI:10.1021/jm0110486
日期:2002.8.1
asymmetric synthesis and biological activity of (2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine 7 and its epimer at the C3' center 6 are described. Compound 7 is a highly potent and selective agonist for group 2 metabotropric glutamate receptors (mGluRs). It is also systemically 4 orders of magnitude more active in the fear-potentiated startle model of anxiety in rats than the rigid constrained