PMID- 2828078 OWN - NLM STAT- MEDLINE DCOM- 19880307 LR - 20190624 IS - 0014-2999 (Print) IS - 0014-2999 (Linking) VI - 142 IP - 3 DP - 1987 Oct 27 TI - Pregnenolone and its sulphate modulate GABAA-receptor-mediated contractile responses in the guinea-pig isolated ileum. PG - 461-4 AB - Pregnenolone and its sulphate had concentration-dependent dual actions on gamma-aminobutyric acid (GABAA)-receptor-mediated ileal contractile responses, enhancing at 0.001-1 microM but inhibiting at 10 microM. There was a sinistral shift of the GABA dose-response curve in the presence of 0.01 microM pregnenolone, with a significant potentiation over the lower concentration range of GABA (3-30 microM), whilst 10 microM pregnenolone depressed the curve by 50% without a significant change in the EC50, in a manner resembling non-competitive inhibition with picrotoxin. Pregnenolone and its sulphate evidently have modulatory actions at ileal GABAA-receptor complexes in keeping with those seen using neurochemical studies in the central nervous system. FAU - Ong, J AU - Ong J AD - Department of Pharmacology, University of Sydney, New South Wales, Australia. FAU - Kerr, D I AU - Kerr DI FAU - Johnston, G A AU - Johnston GA LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PL - Netherlands TA - Eur J Pharmacol JT - European journal of pharmacology JID - 1254354 RN - 0 (Receptors, GABA-A) RN - 04Y4D91RG0 (pregnenolone sulfate) RN - 73R90F7MQ8 (Pregnenolone) SB - IM MH - Animals MH - Female MH - Guinea Pigs MH - Ileum/physiology MH - In Vitro Techniques MH - Male MH - Muscle Contraction/drug effects MH - Muscle, Smooth/*physiology MH - Pregnenolone/*pharmacology MH - Receptors, GABA-A/*physiology EDAT- 1987/10/27 00:00 MHDA- 1987/10/27 00:01 CRDT- 1987/10/27 00:00 PHST- 1987/10/27 00:00 [pubmed] PHST- 1987/10/27 00:01 [medline] PHST- 1987/10/27 00:00 [entrez] AID - 0014-2999(87)90089-6 [pii] AID - 10.1016/0014-2999(87)90089-6 [doi] PST - ppublish SO - Eur J Pharmacol. 1987 Oct 27;142(3):461-4. doi: 10.1016/0014-2999(87)90089-6.