ETA Human Endothelin GPCR Cell Based Antagonist IP1 LeadHunter Assay - TW

Background Information:

The G protein-coupled receptors ETA and ETB are both endothelin receptors whose activation results in the elevation of intracellular-free calcium. ETA is expressed primarily on vascular smooth muscles, mediating vasoconstriction and sodium retention, leading to increased blood pressure. ETB is expressed predominantly on the endothelial surface of vessels, mediating vasodilatation through the production of nitric oxide and prostacyclin. ETA activation has damaging effects on preeclampsia, heart failure, pulmonary hypertension, and kidney natriuresis. Endothelin-receptor antagonists (ERA) can improve exercise capacity, hemodynamics, symptoms, and right ventricle function as an important treatment of hypertension. The selective blockade of ETA blocks only the harmful vasoconstriction effects of ETA but maintains the potential beneficial effects mediated by ETB (vasodilatation and endothelin clearance).

Family:

GPCR

Sub Family:

Endothelin

Class:

Class A

Protein Name:

ETA

Uniprot Number:

P25101

Protein Aliases:

ET-A|ET-AR

Gene Name:

EDNRA

Gene ID:

1909

Accession Number:

S63938

Organism:

Human

Construct Details:

Recombinant

Cell Type:

Chem-1