Golexanolone, also known by the developmental code name GR-3027, is a
neurosteroid
Neurosteroids, also known as neuroactive steroids, are endogenous or exogenous steroids that rapidly alter neuronal excitability through interaction with ligand-gated ion channels and other cell surface receptors. The term ''neurosteroid'' was coin ...
medication which is under development for the treatment of
hypersomnia and
hepatic encephalopathy.
It acts as a
negative allosteric modulator of the
GABAA receptor.
The medication selectively antagonizes the stimulatory actions of
inhibitory neurosteroids like
allopregnanolone
Allopregnanolone is a naturally occurring neurosteroid which is made in the body from the hormone progesterone. As a medication, allopregnanolone is referred to as brexanolone, sold under the brand name Zulresso, and used to treat postpartum d ...
and
tetrahydrodeoxycorticosterone
Tetrahydrodeoxycorticosterone (abbreviated as THDOC; 3α,21-dihydroxy-5α-pregnan-20-one), also referred to as ''allotetrahydrocorticosterone'', is an endogenous neurosteroid. It is synthesized from the adrenal hormone deoxycorticosterone by the ...
(THDOC) at the GABA
A receptor, while not affecting the activation of the GABA
A receptor by
γ-aminobutyric acid (GABA).
See also
*
List of neurosteroids § Excitatory
References
External links
Golexanolone (GR-3027) - AdisInsight
Tertiary alcohols
Ethynyl compounds
Androstanes
Experimental drugs
Ketoximes
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