IP Receptor Antibodies
The classical prostacyclin (IP) receptor is coupled via a Gs protein to stimulation of adenylate cyclase resulting in relaxation of vascular smooth muscle, inhibition of platelet aggregation. Prostacyclin itself is rarely used as a standard IP receptor agonist owing to its instability under physiological conditions. Of the stable prostacyclin analogues available, cicaprost and selexipag are the most selective IP receptor agonists. Treprostinil also shows potent DP1 receptor and EP2 receptor agonism. A large range of non-prostanoid prostacyclin mimetics exists. Selective IP receptor antagonists that competitively block the vasodilator and platelet-inhibitory actions of IP receptor agonists have recently been described. The potential benefits of activation of IP receptors by endogenous prostacyclin in cardiovascular disease has received intense scrutiny of late owing to the tendency of selective COX-2 inhibitors to cause more adverse cardiovascular events than traditional COX-1/COX-2 inhibitors. However, PGI2 may not always have beneficial actions in the body as shown by the ability of IP antagonists to suppress hyperalgesia and oedema in animal models of inflammation. IP receptors are regulated by phosphorylation of carboxyl-terminal serine319/threonine321 (pS319/pT321-IP), serine324/serine328 (pS324/pS328-IP). This nomenclature refers to the human IP receptor. For more information on prostanoid receptor pharmacology please refer to the IUPHAR database. For further reading refer to:
Coleman RA, Smith WL, Narumiya S. International Union of Pharmacology classification of prostanoid receptors: properties, distribution, and structure of the receptors and their subtypes. Pharmacol Rev. 1994 Jun;46(2):205-29. PMID: 7938166.
Woodward DF, Jones RL, Narumiya S. International Union of Basic and Clinical Pharmacology. LXXXIII: classification of prostanoid receptors, updating 15 years of progress. Pharmacol Rev. 2011 Sep;63(3):471-538. doi: 10.1124/pr.110.003517. PMID: 21752876.