Neuroactive steroid modulation of GABAA receptors. 1995

R W Olsen, and D W Sapp
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.

UI MeSH Term Description Entries
D009420 Nervous System The entire nerve apparatus, composed of a central part, the brain and spinal cord, and a peripheral part, the cranial and spinal nerves, autonomic ganglia, and plexuses. (Stedman, 26th ed) Nervous Systems,System, Nervous,Systems, Nervous
D011963 Receptors, GABA-A Cell surface proteins which bind GAMMA-AMINOBUTYRIC ACID and contain an integral membrane chloride channel. Each receptor is assembled as a pentamer from a pool of at least 19 different possible subunits. The receptors belong to a superfamily that share a common CYSTEINE loop. Benzodiazepine-Gaba Receptors,GABA-A Receptors,Receptors, Benzodiazepine,Receptors, Benzodiazepine-GABA,Receptors, Diazepam,Receptors, GABA-Benzodiazepine,Receptors, Muscimol,Benzodiazepine Receptor,Benzodiazepine Receptors,Benzodiazepine-GABA Receptor,Diazepam Receptor,Diazepam Receptors,GABA(A) Receptor,GABA-A Receptor,GABA-A Receptor alpha Subunit,GABA-A Receptor beta Subunit,GABA-A Receptor delta Subunit,GABA-A Receptor epsilon Subunit,GABA-A Receptor gamma Subunit,GABA-A Receptor rho Subunit,GABA-Benzodiazepine Receptor,GABA-Benzodiazepine Receptors,Muscimol Receptor,Muscimol Receptors,delta Subunit, GABA-A Receptor,epsilon Subunit, GABA-A Receptor,gamma-Aminobutyric Acid Subtype A Receptors,Benzodiazepine GABA Receptor,Benzodiazepine Gaba Receptors,GABA A Receptor,GABA A Receptor alpha Subunit,GABA A Receptor beta Subunit,GABA A Receptor delta Subunit,GABA A Receptor epsilon Subunit,GABA A Receptor gamma Subunit,GABA A Receptor rho Subunit,GABA A Receptors,GABA Benzodiazepine Receptor,GABA Benzodiazepine Receptors,Receptor, Benzodiazepine,Receptor, Benzodiazepine-GABA,Receptor, Diazepam,Receptor, GABA-A,Receptor, GABA-Benzodiazepine,Receptor, Muscimol,Receptors, Benzodiazepine GABA,Receptors, GABA A,Receptors, GABA Benzodiazepine,delta Subunit, GABA A Receptor,epsilon Subunit, GABA A Receptor,gamma Aminobutyric Acid Subtype A Receptors
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D013256 Steroids A group of polycyclic compounds closely related biochemically to TERPENES. They include cholesterol, numerous hormones, precursors of certain vitamins, bile acids, alcohols (STEROLS), and certain natural drugs and poisons. Steroids have a common nucleus, a fused, reduced 17-carbon atom ring system, cyclopentanoperhydrophenanthrene. Most steroids also have two methyl groups and an aliphatic side-chain attached to the nucleus. (From Hawley's Condensed Chemical Dictionary, 11th ed) Steroid,Catatoxic Steroids,Steroids, Catatoxic
D018682 GABA Agents Substances used for their pharmacological actions on GABAergic systems. GABAergic agents include agonists, antagonists, degradation or uptake inhibitors, depleters, precursors, and modulators of receptor function. gamma-Aminobutyric Acid Agents,GABA Effect,GABA Effects,GABAergic Agent,GABAergic Agents,GABAergic Effect,GABAergic Effects,Acid Agents, gamma-Aminobutyric,Agent, GABAergic,Agents, GABA,Agents, GABAergic,Agents, gamma-Aminobutyric Acid,Effect, GABA,Effect, GABAergic,Effects, GABA,Effects, GABAergic,gamma Aminobutyric Acid Agents

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