Stereoselective actions of halothane at GABA(A) receptors

European Journal of Pharmacology
B D HarrisP Skolnick

Abstract

Isoflurane anesthesia exhibits stereoselectivity, and a corresponding stereoselectivity ((+)->(-)-isomer) has been reported at GABA(A) receptors in vitro. The objective of the present study was to determine if the positive modulatory actions of halothane at GABA(A) receptors exhibited a similar stereoselectivity. Both (R)- and (S)-halothane ((+)- and (-)- isomers, respectively) enhanced [3H]flunitrazepam binding to brain membranes in a concentration dependent manner without a significant difference in either potency (EC50) or efficacy (Emax). While both (R)- and (S)-halothane enhanced [3H]muscimol binding, the potency of the (+)-isomer was slightly greater than the corresponding (-)-isomer (0.91 +/- 0.17 versus 1.45 +/- 0.04% atmospheres, respectively (P < 0.02)). Thus, subtle structural differences between inhalational anesthetics can have a significant impact on the degree of stereoselectivity at the receptor level and may provide insights for the development of more specific drugs.

References

Mar 1, 1978·Anesthesiology·B WolfsonE S Siker
Jul 7, 1992·European Journal of Pharmacology·B HarrisP Skolnick
Apr 1, 1991·Acta Anaesthesiologica Scandinavica·S NakaoK Mori
Nov 1, 1973·Anesthesiology·J J KendigE N Cohen
Feb 17, 1994·Nature·N P Franks, W R Lieb
Oct 1, 1994·Trends in Pharmacological Sciences·E J MoodyP Skolnick
Sep 22, 1994·European Journal of Pharmacology·G S LyskoR A Ferrone
Oct 11, 1994·Proceedings of the National Academy of Sciences of the United States of America·M M SedenskyP G Morgan
May 17, 1994·European Journal of Pharmacology·B D HarrisP Skolnick

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Citations

Jun 22, 2000·Biomedical Chromatography : BMC·H Y Aboul-EneinJ Szymura-Oleksiak
Oct 19, 2000·Journal of Basic and Clinical Physiology and Pharmacology·M Perouansky, R A Pearce
May 23, 2012·Current Opinion in Anaesthesiology·Edward J Bertaccini, James R Trudell
Jul 18, 2019·Angewandte Chemie·Susanta K NayakGiuseppe Resnati
Jan 27, 2004·The Journal of Pharmacology and Experimental Therapeutics·Eric B GonzalesGlenn H Dillon
Oct 4, 2019·Current Medicinal Chemistry·Yuzhong WangCheng-Pan Zhang

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