Steroid Modulation of GABAA Receptors
作者： J. J. Lambert , J. A. Peters , S. C. Harney , D. Belelli
DOI: 10.1007/978-3-642-56833-6_4
关键词:
摘要: In 1984, Harrison and Simmonds demonstrated the synthetic steroidal anaesthetic alphaxalone (5α-pregnan-3α-ol-ll,20-dione) to enhance potently selectively interaction of γ-aminobutyric acid (GABA) with GABAA receptor (Harrison 1984). same year, steroid hormone androsterone (5α-androstan-3α-ol-17-one) was shown share this activity, albeit reduced potency (Simmonds et al. Alphaxalone are closely related structurally some endogenously occurring metabolites progesterone (i.e. 5α- or 5β-pregnan-3α-ol-20-one) deoxycorticosterone (5α-pregnane-3α,21-diol-20-one) which led logically evaluation such steroids as allosteric modulators function. electrophysiological, tracer-flux radioligand binding studies, were found be more potent than in potentiating action agonists at interactions established sites for other (e.g. benzodiazepines) revealed (Majewska 1986; Callachan 1987; 1987a; Gee 1987, 1988). addition, relatively high concentrations, exerted a direct GABA-mimetic effect (Callachan Cottrell 1987).
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