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Neuroactive steroid modulation of GABAA receptors.

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Department of Molecular and Medical Pharmacology, University of California, Los Angeles 90024-1735, USA.


In summary, the discovery of neuroactive steroids has led to a new appreciation of endocrine-nervous system interactions. The modulation of GABAA receptors by steroid hormone metabolites has far-reaching physiological and pharmacological implications, including relevance to human psychiatric and neurological problems (Fig. 7): I. MECHANISM OF GENERAL ANESTHESIA (Alphaxalone) II. GABA TONE IN SOME REGIONS (e.g., caudate) III. ANTI-ANXIETY ACTIVITY: (Post-partum depression, premenstrual syndrome?) (New drugs?) IV. CHILDBIRTH V. ANTIEPILEPTIC ACTIVITY (New drugs?) VI. REGIONAL HETEROGENEITY (Receptor subtypes) VII. PARTIAL AGONISTS (Better clinical profile?) FIG. 7. Implications of GABAA receptor as a nongenomic CNS target of steroids.

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