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The prostacyclin receptor, also termed the prostaglandin I 2 receptor or just IP, is a receptor belonging to the prostaglandin (PG) group of receptors.IP binds to and mediates the biological actions of prostacyclin (also termed prostaglandin I 2, PGI 2, or when used as a drug, epoprostenol).
Prostacyclin is produced in endothelial cells, which line the walls of arteries and veins, [14] from prostaglandin H 2 (PGH 2) by the action of the enzyme prostacyclin synthase. Although prostacyclin is considered an independent mediator, it is called PGI 2 (prostaglandin I 2 ) in eicosanoid nomenclature, and is a member of the prostanoids ...
They are named based on the prostanoid to which they preferentially bind and respond, e.g. the receptor responsive to PGI2 at lower concentrations than any other prostanoid is named the Prostacyclin receptor (IP). One exception to this rule is the receptor for thromboxane A2 (TP) which binds and responds to PGH2 and TXA2 equally well.
What classifies as later stage in Arena's puny pipeline is APD811, a prostacyclin (IP) receptor agonist for the treatment of pulmonary arterial hypertension, or PAH. In October, Arena announced ...
The following is a comparison of different types of prostaglandin, including prostaglandin I 2 (prostacyclin; PGI 2), prostaglandin D 2 (PGD 2), prostaglandin E 2 (PGE 2), and prostaglandin F 2α (PGF 2α). [19]
PGI2, prostacyclin, binds to IP receptors that catalyze cAMP formation. This process is mediated via GTP-binding protein Gs and adenylyl cyclase. PGE1 binds to IP receptors. IP receptors bind with ionophores that induce ADP and serotonin secretion. PGE1 inhibits the secretion of factors that stimulate platelet aggregation by competitive inhibition.
19223 Ensembl ENSG00000124212 n/a UniProt Q16647 O35074 RefSeq (mRNA) NM_000961 NM_008968 RefSeq (protein) NP_000952 NP_032994 Location (UCSC) Chr 20: 49.5 – 49.57 Mb n/a PubMed search Wikidata View/Edit Human View/Edit Mouse Prostaglandin-I synthase (EC 5.3.99.4) also known as prostaglandin I2 (prostacyclin) synthase (PTGIS) or CYP8A1 is an enzyme involved in prostanoid biosynthesis that in ...
Selexipag, sold under the brand name Uptravi, is a medication developed by Actelion for the treatment of pulmonary arterial hypertension (PAH). [3] [4] Selexipag and its active metabolite, ACT-333679 (or MRE-269, the free carboxylic acid), are agonists of the prostacyclin receptor, which leads to vasodilation in the pulmonary circulation. [5]
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