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Computer-assisted modeling of the picrotoxinin and gamma-butyrolactone receptor site

WE Klunk, BL Kalman, JA Ferrendelli and DF Covey

Three-dimensional models of the picrotoxinin and alkyl-substituted gamma-butyrolactone (GBL) receptor sites were constructed with the aid of a molecular graphics computer system (MMS-X). These two independently derived models proved to be very compatible, which suggested that both types of compounds share a common site of action. Since picrotoxinin is known to act at gamma-aminobutyric acid-regulated chloride channels, a hypothesis was made and tested that the convulsant GBL and picrotoxinin analogues physically impede the passage of chloride ions through the channel. It was also shown that it was theoretically possible for the anticonvulsant GBLs to act at this same site without blocking chloride flux. Finally, the model was applied to several convulsant and anticonvulsant compounds of different chemical classes and was found to be of somewhat general applicability.

Volume 23, Issue 2, pp. 511-518, 03/01/1983
Copyright © 1983 by American Society for Pharmacology and Experimental Therapeutics




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Copyright © 1983 by the American Society for Pharmacology and Experimental Therapeutics