Hypocretin (orexin) receptor 2
Encyclopedia
Orexin receptor type 2 also known as hypocretin receptor type 2, is a protein
that in humans is encoded by the HCRTR2 gene
.
. OX2 binds both orexin
A and orexin B neuropeptides. OX2 is involved in the central feedback mechanism that regulates feeding behaviour.
Protein
Proteins are biochemical compounds consisting of one or more polypeptides typically folded into a globular or fibrous form, facilitating a biological function. A polypeptide is a single linear polymer chain of amino acids bonded together by peptide bonds between the carboxyl and amino groups of...
that in humans is encoded by the HCRTR2 gene
Gene
A gene is a molecular unit of heredity of a living organism. It is a name given to some stretches of DNA and RNA that code for a type of protein or for an RNA chain that has a function in the organism. Living beings depend on genes, as they specify all proteins and functional RNA chains...
.
Function
OX2 is a G-protein coupled receptor expressed exclusively in the brain. It has 64% identity with OX1Hypocretin (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 :...
. OX2 binds both orexin
Orexin
Orexins, also called hypocretins, are the common names given to a pair of excitatory neuropeptide hormones that were simultaneously discovered by two groups of researchers in rat brains....
A and orexin B neuropeptides. OX2 is involved in the central feedback mechanism that regulates feeding behaviour.
Antagonists
- AlmorexantAlmorexantAlmorexant is a competitive receptor antagonist of the OX1 and OX2 orexin receptors, which was being developed by the pharmaceutical companies Actelion and GSK for the treatment of insomnia...
- mixed OX1/2 antagonist - SB-649,868 - mixed OX1/2 antagonist
- TCS-OX2-29TCS-OX2-29TCS-OX2-29 is a drug which was the first non-peptide antagonist developed that is selective for the orexin receptor subtype OX2, with an IC50 of 40nM and selectivity of around 250x for OX2 over OX1 receptors...
- selective OX2 antagonist - 1-(2,4-dibromophenyl)-3-((4S,5S)-2,2-dimethyl-4-phenyl-[1,3]dioxan-5-yl)urea (600x selective for OX2 over OX1)
- (3,4-dimethoxyphenoxy)alkylamino acetamides