Neurosteroids: Endogenous regulators of the GABAA receptor

Delia Belelli; Jeremy J. Lambert

doi:10.1038/nrn1703

Neurosteroids: Endogenous regulators of the GABA_A receptor

Delia Belelli, Jeremy J. Lambert

Systems Medicine

Research output: Contribution to journal › Review article › peer-review

957 Citations (Scopus)

Abstract

GABA_A (γ-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.

Original language	English
Pages (from-to)	565-575
Number of pages	11
Journal	Nature Reviews Neuroscience
Volume	6
Issue number	7
DOIs	https://doi.org/10.1038/nrn1703
Publication status	Published - 15 Jun 2005

ASJC Scopus subject areas

Neuroscience(all)

Access to Document

10.1038/nrn1703

Cite this

@article{6d9ea6880ece4081a2adee78e3923064,

title = "Neurosteroids: Endogenous regulators of the GABAA receptor",

abstract = "GABAA (γ-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 GABAA 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.",

author = "Delia Belelli and Lambert, {Jeremy J.}",

year = "2005",

month = jun,

day = "15",

doi = "10.1038/nrn1703",

language = "English",

volume = "6",

pages = "565--575",

journal = "Nature Reviews Neuroscience",

issn = "1471-003X",

publisher = "Nature Publishing Group",

number = "7",

}

TY - JOUR

T1 - Neurosteroids

T2 - Endogenous regulators of the GABAA receptor

AU - Belelli, Delia

AU - Lambert, Jeremy J.

PY - 2005/6/15

Y1 - 2005/6/15

N2 - GABAA (γ-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 GABAA 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.

AB - GABAA (γ-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 GABAA 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.

U2 - 10.1038/nrn1703

DO - 10.1038/nrn1703

M3 - Review article

C2 - 15959466

AN - SCOPUS:21744447595

SN - 1471-003X

VL - 6

SP - 565

EP - 575

JO - Nature Reviews Neuroscience

JF - Nature Reviews Neuroscience

IS - 7