SB-334,867
Encyclopedia
SB-334,867 is a drug which was the first non-peptide antagonist developed that is selective for the orexin receptor
subtype OX1
, with around 50x selectivity for OX1 over OX2
receptors. It has been shown to produce sedative
and anorectic
effects in animals, and has been useful in characterising the orexinergic regulation of brain systems involved with appetite and sleep, as well as other physiological processes. Orexin antagonists have multiple potential clinical applications including the treatment of drug addiction, insomnia, obesity and diabetes.
Orexin receptor
The orexin receptor is a G-protein-coupled receptor that binds the neuropeptide hormone orexin. There are two variants, OX1 and OX2, each encoded by a different gene .-External links:...
subtype OX1
Hypocretin (orexin) receptor 1
Orexin receptor type 1 , also known as hypocretin receptor type 1, is a protein that in humans is encoded by the HCRTR1 gene.- Function :...
, with around 50x selectivity for OX1 over OX2
Hypocretin (orexin) receptor 2
Orexin receptor type 2 , also known as hypocretin receptor type 2, is a protein that in humans is encoded by the HCRTR2 gene.- Function :...
receptors. It has been shown to produce sedative
Sedative
A sedative or tranquilizer is a substance that induces sedation by reducing irritability or excitement....
and anorectic
Anorectic
An anorectic or anorexic , also known as anorexigenic or appetite suppressant, is a dietary supplement and/or drug which reduces appetite, food consumption, and as a result, causes weight loss to occur.-List of anorectics:Numerous pharmaceutical compounds are marketed as appetite suppressants.The...
effects in animals, and has been useful in characterising the orexinergic regulation of brain systems involved with appetite and sleep, as well as other physiological processes. Orexin antagonists have multiple potential clinical applications including the treatment of drug addiction, insomnia, obesity and diabetes.