Hypocretin (orexin) receptor 1
Encyclopedia
Orexin receptor type 1 also known as hypocretin receptor type 1, is a protein
that in humans is encoded by the HCRTR1 gene
.
and involved in the regulation of feeding behaviour. OX1 selectively binds the orexin-A
neuropeptide. It shares 64% identity with OX2
.
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 HCRTR1 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
The orexin 1 receptor (OX1), is a G-protein coupled receptor expressed in the hypothalamusHypothalamus
The Hypothalamus is a portion of the brain that contains a number of small nuclei with a variety of functions...
and involved in the regulation of feeding behaviour. OX1 selectively binds the orexin-A
Orexin-A
Orexin A, also known as Hypocretin-1, is a naturally occurring, highly excitatory, neuropeptide released by the hypothalamus. As a pharmaceutical drug, Orexin A is most commonly administered as a nasal spray...
neuropeptide. It shares 64% identity with 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 :...
.
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-334,867SB-334,867SB-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...
- selective OX1 antagonist - SB-408,124SB-408,124SB-408,124 is a drug which is a non-peptide antagonist selective for the orexin receptor subtype OX1, with around 70x selectivity for OX1 over OX2 receptors, and improved oral bioavailability compared to the older OX1 antagonist SB-334,867. It is used in scientific research into the function of...
- selective OX1 antagonist - SB-649,868 - mixed OX1/2 antagonist