Article date: 1985/2/1
PubMed ID: 2982013
Journal name: The Journal of pharmacology and experimental therapeutics (ISSN: 0022-3565)
Pantoyl-gamma-aminobutyric acid (P-GABA) administered i.p. inhibited scopolamine- and atropine-induced locomotor activities in mice, but did not inhibit methamphetamine- and apomorphine-induced locomotor activities. In radiolabeled ligand binding experiments, P-GABA did not inhibit the bindings of [3H]quinuclidinyl benzilate, [3H]spiroperidol and [3H]apomorphine to rat brain membranes, but inhibited that of [3H]muscimol. GABA and P-GABA enhanced K+ (25 mM)-induced release of [3H]acetylcholine from slices of the cerebral cortex and hippocampus dose-dependently, and their effects were antagonized by bicuculline but not by tetrodotoxin. These results suggest that P-GABA binds to GABA receptors causing enhanced cholinergic neurotransmission in the central nervous system. The results are discussed in relation to the clinical use of P-GABA in treatment of Alzheimer's disease and senile dementia of the Alzheimer type.
Author List: Nakahiro M, Fujita N, Fukuchi I, Saito K, Nishimura T, Yoshida H
Publication Types: Journal Article; Research Support, Non-U.S. Gov't
Substances mentioned in the article: Receptors, GABA-A; pantogab; Pantothenic Acid; gamma-Aminobutyric Acid; Acetylcholine;
Mesh terms: Acetylcholine/metabolism; Animals; Brain/drug effects; Female; Male; Mice; Mice, Inbred ICR; Motor Activity/drug effects; Pantothenic Acid/analogs & derivatives; Parasympathetic Nervous System/drug effects; Rats; Rats, Inbred Strains; Receptors, GABA-A/drug effects; Synaptic Transmission/drug effects; gamma-Aminobutyric Acid/analogs & derivatives;