Prostacyclin receptor
| Prostacyclin receptor | ||
|---|---|---|
| Properties of human protein | ||
| Mass / length primary structure | 383 amino acids | |
| Secondary to quaternary structure | multipass receptor | |
| Identifier | ||
| Gene name | PTGIR | |
| External IDs | ||
| Occurrence | ||
| Parent taxon | Vertebrates | |
The prostacyclin receptor (or IP receptor for short ) is a cell membrane-bound G-protein-coupled receptor in vertebrates that mediates the effects of prostacyclin . It belongs to the upper group of prostaglandin receptors .
Among other things, it mediates the following effects of prostacyclin :
- the pain-intensifying effect of prostacyclin on sensitive nerves (like the EP1 receptor mediates the pain-intensifying effect of PGE 2 ).
- the inhibition of gastric acid secretion (like the EP3 receptor for the PGE 2 ).
- the inhibition of vascular smooth muscle cell contraction with vasodilation .
- inhibition of thrombus formation in platelets .
Agonist
Selexipag is an oral selective receptor agonist . By activating the prostacyclin receptor, it can trigger a vasodilation in the pulmonary arterial circulation, normally mediated by prostacyclin , which can lower the blood pressure in pulmonary hypertension . A French multicentre, randomized, double-blind, placebo- controlled clinical phase III study ("GRIPHON study") with 1,156 patients showed a significant positive effect with a hazard ratio of 0.60 under selexipag (the primary endpoint was 27.0% under Selexipag and achieved in 41.6% with placebo).
Individual evidence
- ↑ Homologues at OMA
- ↑ Olivier Sitbon, Richard Channick et al .: Selexipag for the treatment of pulmonary arterial hypertension . New England Journal of Medicine 2015, Volume 373, Issue 26, December 24, 2015, Pages 2522-2533, DOI: 10.1056 / NEJMoa1503184