Introduction
Major types of Prostanoid Receptor
E-type prostanoid (EP) receptors are an important class of prostanoid receptor, termed EP1, EP2, EP3 and EP4. EP1 was the first reported EP receptor and was found in kidney and lung tissue at a low level. The human EP1 receptor is composed of 402 amino acids, sharing a sequence homology of 86% with the rat EP1 receptor. EP2 and EP4 have the similarities in pharmacology and functional coupling, mediating celluar signaling via adenylate cyclase activity. The EP3 receptor is reported to have various isoforms that differ in the amino acid sequence of the C-terminal region.
Agonists/antagonists of Prostanoid Receptor
It’s obvious that the development of potent and selective agonists and antagonists of EP receptor is required for the research in prostanoid biology. ONO-DI-004, a derivate of PGE, is selective EP1 receptor agonist with moderate affinity with the receptor. ONO-8711 is a competitive EP1 receptor antagonist, inhibiting the increase of cytosolic Ca2+ concentration. Recently, more selective and potent EP2 receptor antagonists have been synthesized, such as AH-6809, PF-04418948, TG6-129, and TG4-155. There are many agonists and antagonists against the EP3 receptors developed due to the huge amount of EP3 isoforms. Commercially available EP4 agonists and antagonists have emerged since 2000.
E-type prostanoid (EP) receptors are an important class of prostanoid receptor, termed EP1, EP2, EP3 and EP4. EP1 was the first reported EP receptor and was found in kidney and lung tissue at a low level. The human EP1 receptor is composed of 402 amino acids, sharing a sequence homology of 86% with the rat EP1 receptor. EP2 and EP4 have the similarities in pharmacology and functional coupling, mediating celluar signaling via adenylate cyclase activity. The EP3 receptor is reported to have various isoforms that differ in the amino acid sequence of the C-terminal region.
Agonists/antagonists of Prostanoid Receptor
It’s obvious that the development of potent and selective agonists and antagonists of EP receptor is required for the research in prostanoid biology. ONO-DI-004, a derivate of PGE, is selective EP1 receptor agonist with moderate affinity with the receptor. ONO-8711 is a competitive EP1 receptor antagonist, inhibiting the increase of cytosolic Ca2+ concentration. Recently, more selective and potent EP2 receptor antagonists have been synthesized, such as AH-6809, PF-04418948, TG6-129, and TG4-155. There are many agonists and antagonists against the EP3 receptors developed due to the huge amount of EP3 isoforms. Commercially available EP4 agonists and antagonists have emerged since 2000.
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