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Type: Journal article
Title: Evaluation of 3-aminopropanesulphonamide analogues of GABA as antagonists at GABA (B) receptors in peripheral and central preparations
Author: Ong, J.
Kerr, D.
Bowden, J.
Prager, R.
Citation: European Journal of Pharmacology, 1999; 367(2-3):207-211
Issue Date: 1999
ISSN: 0014-2999
Abstract: Cholinergic twitch responses in the guinea-pig isolated ileum, and spontaneous discharges in rat neocortical slices, were depressed by the GABA(B) receptor agonist baclofen. These actions were reversibly antagonised by the sulphonamide derivatives (R,S)-2-hydroxy-3-phthalimidopropanesulphonamide (HPIPS), 3-amino-N-benzoylpropanesulphonamide (ABPS) and 3-phthalimidopropanesulphonamide (PIPS) which produced rightwards shifts of the baclofen concentration-response curves, with pA2 values ranging between 4.1 and 4.3 in both preparations. From these results, HPIPS, ABPS and PIPS constitute a novel class of antagonists at GABA(B) hetero-receptors.
Keywords: Muscle, Smooth; Ileum; Neocortex; Animals; Guinea Pigs; Rats; Rats, Sprague-Dawley; Sulfonamides; gamma-Aminobutyric Acid; Baclofen; GABA Agonists; GABA Antagonists; Drug Interactions; Male; GABA-B Receptor Antagonists; In Vitro Techniques
RMID: 0030006085
DOI: 10.1016/S0014-2999(98)00962-5
Appears in Collections:Anaesthesia and Intensive Care publications

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