Discovery of non-Zwitterionic GABA A receptor full agonists and a superagonist

…, ESH Chow, RL Barlow, JR Bloomquist

Index: Carlier, Paul R; Chow, Ella S-H; Barlow, Rebecca L; Bloomquist, Jeffrey R Bioorganic and medicinal chemistry letters, 2002 , vol. 12, # 15 p. 1985 - 1988

Full Text: HTML

Citation Number: 15

Abstract

Numerous previous studies of GABAA receptor ligands have suggested that GABAA receptor agonists must be zwitterionic and feature an intercharge separation similar to that of GABA (approx. 4.7–6Å). In this communication we demonstrate that appropriately functionalized GABA amides are partial, full, or superagonists, despite their non-zwitterionic structure.

Related Articles:

A convenient and general method for the preparation of tert-butoxycarbonylaminoalkanenitriles and their conversion to mono-tert-butoxycarbonylalkanediamines

[Houssin, Raymond; Bernier, Jean-Luc; Henichart, Jean-Pierre Synthesis, 1988 , # 3 p. 259 - 261]

Decarboxylative reduction of free aliphatic carboxylic acids by photogenerated cation radical

[Yoshimi, Yasuharu; Itou, Tatsuya; Hatanaka, Minoru Chemical Communications, 2007 , # 48 p. 5244 - 5246]

Mapping of the active site of rat kidney γ-glutamyl transpeptidase using activated esters and their amide derivatives

[Castonguay, Roselyne; Lherbet, Christian; Keillor, Jeffrey W. Bioorganic and Medicinal Chemistry, 2002 , vol. 10, # 12 p. 4185 - 4191]

Mapping of the active site of rat kidney γ-glutamyl transpeptidase using activated esters and their amide derivatives

[Castonguay, Roselyne; Lherbet, Christian; Keillor, Jeffrey W. Bioorganic and Medicinal Chemistry, 2002 , vol. 10, # 12 p. 4185 - 4191]

More Articles...