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https://hdl.handle.net/2440/5983
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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 |
Publisher: | Elsevier BV |
Issue Date: | 1999 |
ISSN: | 0014-2999 1879-0712 |
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 |
DOI: | 10.1016/S0014-2999(98)00962-5 |
Published version: | http://dx.doi.org/10.1016/s0014-2999(98)00962-5 |
Appears in Collections: | Anaesthesia and Intensive Care publications Aurora harvest 5 |
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