PMID: 37300May 1, 1979

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

The Journal of Pharmacy and Pharmacology
J ArntP Krogsgaard-Larsen

Abstract

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.

References

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Citations

Apr 1, 1976·The Journal of Pharmacy and Pharmacology·A Dray, D W Straughan
Mar 1, 1977·The Journal of Pharmacy and Pharmacology·T A James, M S Starr
Jul 7, 1977·Nature·P Krogsgaard-LarsenD R Curtis
Jan 1, 1975·Journal of Neurochemistry·G A JohnstonB Twitchin
Jun 15, 1977·European Journal of Pharmacology·C OberlanderJ R Boissier
May 16, 1975·Brain Research·D TarsyC D Marsden
Dec 1, 1975·Journal of Neurochemistry·P Krogsgaard-LarsenR M McCulloch
Dec 18, 1975·Nature·G A JohnstonA L Stephanson
Jan 1, 1976·Experimental Neurology·J S MendezK E Dahl
Oct 8, 1971·Brain Research·D R CurtisH McLennan
Feb 1, 1973·Journal of Neurochemistry·P M Beart, G A Johnston
Oct 1, 1964·British Journal of Pharmacology and Chemotherapy·J M CRAWFORD, D R Curtis

Related Concepts

Substantia Nigra Structure
Receptors, Drug
Muscimol
Gamma-Aminobutyric Acid, Zinc Salt (2:1)
Stereotyped Behavior
ABAT
Injectables
Munchnones

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