3-Amino-2-hydroxy-N-(4-nitrophenyl)-propanesulphonamide, a new class of GABAB receptor antagonist in central and peripheral preparations
Date
1995
Authors
Kerr, D.
Ong, J.
Hughes, R.
Prager, R.
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Journal article
Citation
European Journal of Pharmacology, 1995; 294(1):349-352
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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.