OX2 Human Orexin GPCR Cell Based Antagonist Arrestin LeadHunter Assay - US

Background Information:

Orexins, also called hypocretins, are the common names given to a pair of highly excitatory neuropeptide hormone. Two highly-related peptides (Orexin A and B) are produced by cleavage of a single precursor protein. Both peptides bind to two G-protein coupled receptors, orexin-1 (OX1) and orexin-2 (OX2). The orexin receptors are located predominantly in the hypothalamus and locus coeruleus, but are also found elsewhere in the CNS. The orexins have been linked to a range of physiological functions including the control of feeding and energy metabolism, modulation of neuroendocrine function, and regulation of the sleep-wake cycle. Orexin OX2 receptor antagonism may be useful for the treatment of insomnia and obesity.

PathHunter β-Arrestin GPCR cell lines are engineered to co-express the ProLink™ (PK) tagged GPCR and the Enzyme Acceptor (EA) tagged β-Arrestin. Activation of the GPCR-PK induces β-Arrestin-EA recruitment, forcing complementation of the two enzyme fragments. The resulting functional enzyme hydrolyzes substrate to generate a chemiluminescent signal. PathHunter cell lines expressing Gq-coupled receptors can also be used to detect calcium mobilization.

Family:

GPCR

Sub Family:

Orexin

Class:

Class A

Coupling:

Gq

Protein Name:

OX2

Uniprot Number:

O43614

Protein Aliases:

orexin receptor 2

Gene Name:

HCRTR2

Gene ID:

3062

Gene Aliases:

OX2R

Accession Number:

AF041245

Organism:

Human

Cell Type:

CHO-K1