Identification of prostaglandin E receptor ‘EP2’ cloned from mastocytoma cells as EP4 subtype

The mouse prostaglandin E receptor EP2 subtype: cloning, expression, and Northern blot analysis

“…As shown in Fig. 2c, specific [3H]PGE2 binding was also inhibited by several ligands in the order of 16,16-dimethyl-PGE2 (a nonselective EP agonist) [6,11] > 11-deoxy PGE~ (an EP2, EP3, and EP4 agonist) [6,11] > misoprostol (an EPz, EP3, and EP4 agonist) [10,20,21] > 1-OH-PGE~ (an EP4 partial agonist) [6] > 19(R)OH-PGE 2 (an EP 2 agonist) [11,22]. This binding characteristic was in good agreement with that of the human EP2 receptor [11], except for the poor reactivity of 19(R)OH-PGE2 to the mouse receptor.…”

“…Pharmacological studies suggested that there are "our subtypes of PGE receptors, EP1, EP2, EP3 and EP 4, which ire thought to differ in their signal transduction mechanisms; :hey are presumed to be coupled to Ca 2+ mobilization, and the ~timulation, inhibition, and stimulation of adenylate cyclase, respectively [3 5]. Among the four subtypes, EP2 and EP 4 are :oupled to the same signal transduction pathway, stimulation af adenylate cyclase, but differ in their activities induced by some ligands including butaprost and AH23848B [5][6][7]. While EP2 is sensitive to butaprost, EP4 is insensitive to butaprost but *Corresponding author.…”

What is the cellular source of prostaglandins in the brain in response to systemic inflammation? Facts and controversies

“…The most recently identified subtype, EP 4 , is like the EP 2 receptor positively coupled to adenylate cyclase. 39,40 We have recently observed a very distinct pattern of EP 2 and EP 4 expression in the rat brain under both basal and immune-challenged conditions and underlined the possible role of the EP 4 subtype in mediating the effects of PGE 2 on different autonomic and neuroendocrine functions. 41 The presence of Fos-ir nuclei in various populations of EP 4 neurons of IL-1-treated animals clearly supports this concept and suggests that the selectivity of the neuronal response during systemic inflammation may depend on the expression of specific PGE 2 receptors in key structures of the brain.…”

A specific prostaglandin E2 receptor and its role in modulating salivary secretion in the female tick, Amblyomma americanum (L.)

“…These four PGE receptor subtypes have been cloned from various tissues (Sugimoto et al, 1992;Honda et al, 1993;Watabe et al, 1993;Adam et al, 1994;Breyer et al, 1994;Nam.ha et al, 1994;Regan et al, 1994;Sando et al, 1994;Yang et al, 1994;Nishigaki et al, 1995). The molecular structures show that they contain seven hydrophobic segments corresponding to the putative transmembrane domains, suggesting that they belong to the family of G protein-coupled rhodopsin-type receptors Narumiya, 1996).…”