The actions of the steroidal convulsant RU 5135 on glycine and GABA sub(A) receptors

The amidine steroid RU 5135 (3 alpha -hydroxy-16-imino-5 beta -17-aza-androstan-11-one) is a potent convulsant which has been reported to bind to both GABA and glycine recognition sites in radioligand binding studies. The present report describes the effects of RU 5135 upon GABA- and glycine-induced...

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Published inBritish Journal of Pharmacology [BR. J. PHARMACOL.]. Vol. 90, no. suppl. 1987 Vol. 90; p. no. sul.
Main Authors Callachan, H, Lambert, J J, Peters, JA
Format Conference Proceeding
LanguageEnglish
Published 01.01.1987
Subjects
glycine
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Summary:The amidine steroid RU 5135 (3 alpha -hydroxy-16-imino-5 beta -17-aza-androstan-11-one) is a potent convulsant which has been reported to bind to both GABA and glycine recognition sites in radioligand binding studies. The present report describes the effects of RU 5135 upon GABA- and glycine-induced currents, recorded under voltage-clamp, from bovine chromaffin cells and murine spinal neurones in culture. RU 5135 is a potent antagonist of responses mediated both by GABA and glycine receptors, and its GABA antagonist properties contrast with the GABA potentiating actions of some steroids.
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ISSN:0007-1188