Muscimol and related GABA receptor agonists: the potency of GABAergic drugs in vivo determined after intranigral injection.

Article date: 1979/5/1

PubMed ID: 37300

Journal name: The Journal of pharmacy and pharmacology (ISSN: 0022-3573)


Contralateral turning behaviour following unilateral intranigral injection of a large series of GABA analogues was investigated. The results indicated that the turning behaviour was induced stereospecifically and was selectively antagonized by the GABA antagonist bicuculline methochloride. The comparative potencies of a series of GABA agonists related to muscimol in general corresponded well to the affinity for 3H-GABA receptor sites and to the depressant action on single neurons using microelectrophoretic administration. However, the GABA agonists trans-aminocrotonic acid and 3-aminopropanesulphonic acid were much weaker than expected from in vitro studies. The GABA-uptake inhibitors nipecotic acid and guvacine showed only weak and short-lasting effects. The GABA-transaminase inhibitor gamma-acetylenic GABA showed delayed effects compared with the agonists which acted immediately. It is proposed that this behavioural effect may be a sensitive and quantitative method for evaluation of GABA agonists in vivo.

This document is available from: http://directlinks.cc/files/muscimol/37300.pdf

Author List: Arnt J, Scheel-Krüger J, Magelund G, Krogsgaard-Larsen P

Publication Types: Journal Article

Substances mentioned in the article: Oxazoles; Receptors, Drug; Muscimol; gamma-Aminobutyric Acid;

Mesh terms: Animals; Humans; Injections; Male; Muscimol/administration & dosage; Oxazoles/pharmacology; Rats; Receptors, Drug/physiology; Stereotyped Behavior/drug effects; Substantia Nigra; Time Factors; gamma-Aminobutyric Acid/physiology;

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