Prostaglandins (PG's) are produced by the metabolism of arachidonic acid. PGE-2 is one of the five physiologically significant prostanoids known. ItÕs wide spectrum of physiologic and pharmacologic effects in various tissues are mediated through binding to the PGE-2 receptors (EP1, EP2, EP3 & EP4). These include effects on the immune, endocrine, cardiovascular, renal and reproductive systems as well as smooth muscle. It is also one of the most abundant of the prostanoid family in the brain where it plays an important role in many neural functions, particularly in newborn babies, and as a mediator of inflammation. _x000B__x000B_PGE-2 signals through a family of G-protein coupled receptors known as EP receptors. There are 4 subtypes of EP receptors, known as EP1, EP2, EP3 and EP4. EP2 receptors are 358 amino acid proteins with a short third intracellular loop. EP2 receptors stimulate adenylyl cyclase by their coupling to Gs and do not undergo PGE-2-induced internalization. EP3 receptors are 365-425 amino acid proteins. There are currently 4 known isoforms of EP3 receptors named EP3A, 3B, 3C and 3D. EP3 receptors are involved in water absorption, gastric acid secretion, uterine contraction, neurotransmitter release and the hydrolysis of fat cells (lipolysis) and also act as a mediator of neural inflammation.
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