Neurosteroids: endogenous regulators of the GABA(A) receptor.
GABA(A) (gamma-aminobutyric acid type A) receptors mediate most of the 'fast' synaptic inhibition in the mammalian brain and are targeted by many clinically important drugs. Certain naturally occurring pregnane steroids can potently and specifically enhance GABA(A) receptor function in a nongenomic (direct) manner, and consequently have anxiolytic, analgesic, anticonvulsant, sedative, hypnotic and anaesthetic properties. These steroids not only act as remote endocrine messengers, but also can be synthesized in the brain, where they modify neuronal activity locally by modulating GABA(A) receptor function. Such 'neurosteroids' can influence mood and behaviour in various physiological and pathophysiological situations, and might contribute to the behavioural effects of psychoactive drugs.
Belelli
Delia
D
Neurosciences Institute, Division of Pathology and Neuroscience, Ninewells Hospital and Medical School, Dundee University, Dundee DD19SY, UK.
Lambert
Jeremy J
JJ
D000818:Animals; D014150:Antipsychotic Agents / Q000627:therapeutic use; D001921:Brain / Q000378:metabolism; D006801:Humans; D008954:Models, Biological; D019964:Mood Disorders / Q000188:drug therapy; D009433:Neural Inhibition / Q000502:physiology; D011278:Pregnanes / Q000737:chemistry / Q000378:metabolism*; D011963:Receptors, GABA-A / Q000378:metabolism* / Q000502:physiology; D009435:Synaptic Transmission / Q000502:physiology
D014150:Antipsychotic Agents; D011278:Pregnanes; D011963:Receptors, GABA-A