Introduction
Endothelin receptor type A is also known as ETA. It is encoded by the EDNRA gene. The EDNRA gene encodes the receptor for endothelin-1, a peptide that plays a role in potent and long-lasting vasoconstriction. This receptor associates with guanine-nucleotide-binding (G) proteins, and this coupling activates a phosphatidylinositol-calcium second messenger system. Polymorphisms in this gene have been linked to migraine headache resistance. Alternative splicing results in multiple transcript variants. [provided by RefSeq, Oct 2009]
Direction of Drugs Discovery
• EDNRA Antagonist
• EDNRA Modulator
• EDNRA Inhibitor
• EDNRA Agonist
• Developing New Clinical Effects on EDNRA from Existing Drugs
Drugs
• EDNRA Antagonist- Ambrisentan, LU302146, clazosentan, atrasentan, darusenta
• EDNRA Modulator- Bosentan, macitentan, PD-145065, BMS-193884, J-104132
• EDNRA Inhibitor- ET-1, BMS-182874, Ac-bhg-F-N-Y-Y-W, PD-163140, W-F-F-N--Y-Y-W
• EDNRA Agonist- Sarafotoxin S6b