3-Amino-2-hydroxy-N-(4-nitrophenyl)-propanesulphonamide, a new class of GABAB receptor antagonist in central and peripheral preparations

Kerr, D.Ong, J.Hughes, R.Prager, R.2006-06-232006-06-231995European Journal of Pharmacology, 1995; 294(1):349-3520014-29991879-0712http://hdl.handle.net/2440/5987Racemic 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.enMuscle, SmoothIleumCentral Nervous SystemCerebral CortexPeripheral Nervous SystemParasympathetic Nervous SystemAnimalsGuinea PigsRatsRats, Sprague-DawleyMagnesiumSulfonamidesBaclofenGABA AgonistsElectric StimulationMuscle ContractionMaleGABA-B Receptor AgonistsGABA-B Receptor AntagonistsIn Vitro Techniques3-Amino-2-hydroxy-N-(4-nitrophenyl)-propanesulphonamide, a new class of GABAB receptor antagonist in central and peripheral preparationsJournal article0030006081001995045610.1016/0014-2999(95)00688-52-s2.0-002956181270087Ong, J. [0000-0002-0958-460X]