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  • Title: Pharmacological characterisation of multiple components in the enhancement by pregnanolone and propofol of [3H]flunitrazepam binding to GABAA receptors.
    Author: Zhong Y, Simmonds MA.
    Journal: Neuropharmacology; 1996; 35(9-10):1193-8. PubMed ID: 9014134.
    Abstract:
    The enhancement by pregnanolone (5 beta-pregnan-3 alpha-ol-20-one) and propofol (2,6-diisopropylphenol) of [3H]flunitrazepam (FNZ) binding to GABAA receptors in rat whole brain homogenate has been investigated. Two components in the concentration-effect relationship for pregnanolone were distinguished by the sensitivity of one component to antagonism by bicuculline and enhancement by muscimol, and the selective but weak antagonism of the bicuculline-insensitive component by 11-ketoprogesterone (4-pregnen-3,11,20-trione). Unlike pregnanolone, the enhancement by propofol of [3H]FNZ binding appeared to comprise a single component which was insensitive to 11-ketoprogesterone and was only slightly antagonised by bicuculline and slightly enhanced by muscimol. These results provide evidence for distinct GABA-dependent and GABA-independent components of the action of pregnanolone in the enhancement of [3H]FNZ binding, with the GABA-independent component being sensitive to 11-ketoprogesterone. The data also support the suggestion of different binding sites for pregnanolone and propofol.
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