V1A Human Vasopressin / Oxytocin GPCR Cell Based Agonist Arrestin LeadHunter Assay - US

Background Information:

Vasopressin receptors belong to the superfamily of G protein-coupled seven transmembrane proteins. G-protein-coupled receptors constitute one of the major signal transduction systems in eukaryotic cells. Coding sequences for these receptors, in those regions believed to contribute to the agonist-antagonist binding site, are strongly conserved across mammalian species. Vasopressin receptors are currently classified into V1A, V1B (V3) and V2 subtypes. The V1A receptor, the most widespread vasopressin receptor subtype, is found in many central nervous system structures and peripheral tissues. Vasopressin V1A receptor agonism may cause hypertension and coronary vasospasm as well as increase platelet aggregation and vascular smooth muscle cell proliferation. Receptor antagonism may be useful in the treatment of dysmenorrhea and Raynaud’s disease.

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:

Vasopressin and Oxytocin

Class:

Class A

Coupling:

Gq

Protein Name:

V1A

Uniprot Number:

P37288

Protein Aliases:

AVPR V1a|Antidiuretic hormone receptor 1a|Vascular/hepatic-type arginine vasopressin receptor

Gene Name:

AVPR1A

Gene ID:

552

Gene Aliases:

AVPR1

Accession Number:

NM_000706.3

Organism:

Human

Cell Type:

U2OS