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3-amino-2-hydroxy-N-(4-nitrophenyl)-propanesulphonamide, a new class of GABAB receptor antagonist in central and peripheral preparations.
- Source :
-
European journal of pharmacology [Eur J Pharmacol] 1995 Dec 27; Vol. 294 (1), pp. 349-52. - Publication Year :
- 1995
-
Abstract
- Racemic 3-amino-2-hydroxy-N-(4-nitrophenyl)-propanesulphonamide (AHPNS), a sulphonamide analog of GABA, reversibly and competitively antagonised the concentration-dependent depression of cholinergic twitch contractions by baclofen, in the electrically stimulated guinea-pig isolated ileum, with a pA2 of 4.0 +/- 0.2. In the rat neocortex, maintained in Mg(2+)-free medium, AHPNS (100-500 microM) also reversibly antagonised the baclofen (10 microM)-induced suppression of spontaneous discharges. AHPNS is a new class of GABAB receptor antagonist that has central and peripheral blocking actions.
- Subjects :
- Animals
Baclofen antagonists & inhibitors
Baclofen pharmacology
Cerebral Cortex drug effects
Cerebral Cortex metabolism
Electric Stimulation
GABA Agonists pharmacology
GABA-B Receptor Agonists
Guinea Pigs
Ileum drug effects
In Vitro Techniques
Magnesium physiology
Male
Muscle Contraction drug effects
Muscle, Smooth drug effects
Parasympathetic Nervous System drug effects
Rats
Rats, Sprague-Dawley
Central Nervous System drug effects
GABA-B Receptor Antagonists
Peripheral Nervous System drug effects
Sulfonamides pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 0014-2999
- Volume :
- 294
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- European journal of pharmacology
- Publication Type :
- Academic Journal
- Accession number :
- 8788452
- Full Text :
- https://doi.org/10.1016/0014-2999(95)00688-5