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|Title:||Evaluation of 3-aminopropanesulphonamide analogues of GABA as antagonists at GABA (B) receptors in peripheral and central preparations|
|Citation:||European Journal of Pharmacology, 1999; 367(2-3):207-211|
|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|
|Appears in Collections:||Anaesthesia and Intensive Care publications|
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