Please use this identifier to cite or link to this item: http://hdl.handle.net/2440/5987
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Type: Journal article
Title: 3-Amino-2-hydroxy-N-(4-nitrophenyl)-propanesulphonamide, a new class of GABAB receptor antagonist in central and peripheral preparations
Author: Kerr, D.
Ong, J.
Hughes, R.
Prager, R.
Citation: European Journal of Pharmacology, 1995; 294(1):349-352
Publisher: North Holland
Issue Date: 1995
ISSN: 0014-2999
1879-0712
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.
Keywords: Muscle, Smooth; Ileum; Central Nervous System; Cerebral Cortex; Peripheral Nervous System; Parasympathetic Nervous System; Animals; Guinea Pigs; Rats; Rats, Sprague-Dawley; Magnesium; Sulfonamides; Baclofen; GABA Agonists; Electric Stimulation; Muscle Contraction; Male; GABA-B Receptor Agonists; GABA-B Receptor Antagonists; In Vitro Techniques
RMID: 0030006081
DOI: 10.1016/0014-2999(95)00688-5
Appears in Collections:Anaesthesia and Intensive Care publications

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