(.+-.)-trans-2-(Aminomethyl)cyclobutanecarboxylic acid hydrochloride: a rigid analog of .gamma.-aminobutyric acid
- 1 October 1980
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 23 (10) , 1142-1144
- https://doi.org/10.1021/jm00184a017
Abstract
The (.+-.) title compound was prepared to evaluate prior observations that certain GABA congeners in the transoid disposition demonstrate GABA receptor binding activity. It was prepared by a multistep sequence from (.+-.)-methyl trans-2-(hydroxymethyl)cyclobutanecarboxylate. In a sodium-independent binding assay, the specific binding of (.+-.)-1 to synaptic membranes prepared from rat brain tissue was 1/14,500 that of GABA.This publication has 6 references indexed in Scilit:
- The Synthesis and Activity of cis‐and trans‐2‐(Aminomethyl) cyclopropanecarboxylic Acid as Conformationally Restricted Analogues of GABAJournal of Neurochemistry, 1980
- GABA analogues: conformational analysis of effects on [3H]GABA binding to postsynaptic receptors in human cerebellumJournal of Neurochemistry, 1979
- GAMMA‐AMINOBUTYRIC ACID BINDING IN MAMMALIAN BRAIN: RECEPTOR‐LIKE SPECIFICITY OF SODIUM‐INDEPENDENT SITESJournal of Neurochemistry, 1978
- STRUCTURE‐ACTIVITY STUDIES ON THE INHIBITION OF GABA BINDING TO RAT BRAIN MEMBRANES BY MUSCIMOL AND RELATED COMPOUNDSJournal of Neurochemistry, 1978
- Effects of some conformationally restricted GABA analogues on GABA membrane binding and nerve ending transportBrain Research, 1978
- INFLUENCES OF IONS, ENZYMES, AND DETERGENTS ON GAMMA-AMINOBUTYRIC ACID RECEPTOR BINDING IN SYNAPTIC-MEMBRANES OF RAT-BRAIN1977