NCS-382
Encyclopedia
NCS-382 is a moderately selective antagonist
for the GHB receptor
. It blocks the effects of GHB
in animals and has both anti-sedative
and anticonvulsant
effects. It has been proposed as a treatment for GHB overdose in humans, as well as for the endogenous metabolic disorder succinic semialdehyde dehydrogenase deficiency
, but has never been developed for clinical use.
Receptor antagonist
A receptor antagonist is a type of receptor ligand or drug that does not provoke a biological response itself upon binding to a receptor, but blocks or dampens agonist-mediated responses...
for the GHB receptor
GHB receptor
Gamma-hydroxybutyrate receptor or GHB receptor , originally identified as GPR172A, is a G protein-coupled receptor that binds gamma-Hydroxybutyric acid .-History:...
. It blocks the effects of GHB
Gamma-Hydroxybutyric acid
γ-Hydroxybutyric acid , also known as 4-hydroxybutanoic acid and sodium oxybate when used for medicinal purposes, is a naturally occurring substance found in the central nervous system, wine, beef, small citrus fruits, and almost all animals in small amounts. It is also categorized as an illegal...
in animals and has both anti-sedative
Sedative
A sedative or tranquilizer is a substance that induces sedation by reducing irritability or excitement....
and anticonvulsant
Anticonvulsant
The anticonvulsants are a diverse group of pharmaceuticals used in the treatment of epileptic seizures. Anticonvulsants are also increasingly being used in the treatment of bipolar disorder, since many seem to act as mood stabilizers, and in the treatment of neuropathic pain. The goal of an...
effects. It has been proposed as a treatment for GHB overdose in humans, as well as for the endogenous metabolic disorder succinic semialdehyde dehydrogenase deficiency
Succinic semialdehyde dehydrogenase deficiency
Succinic semialdehyde dehydrogenase deficiency , also known as 4-hydroxybutyric aciduria or gamma-hydroxybutyric aciduria, is a rare autosomal recessive disorder of the degradation pathway of the inhibitory neurotransmitter γ-aminobutyric acid, or GABA...
, but has never been developed for clinical use.