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Chemical Compound Review

AC1NSK8W     7-[(1R,2S)-2-[(E,3S)-3- hydroxy-4-phenoxy...

Synonyms: LS-58019, MB-28767, PDSP2_001534, MB 28767, M&B-28767, ...
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Disease relevance of Dpt-prostaglandin E1


High impact information on Dpt-prostaglandin E1

  • Mucin secretion and [cAMP](i) production by LS174T cells were stimulated dose-dependently by PGE(2), the EP(4)-receptor agonist 1-OH-PGE(1), and the EP(3)/EP(4) agonist M&B28767 and were inhibited with the adenylate cyclase inhibitor SQ22536 [5].
  • The cytosolic level and secretion of MMP-9 were increased maximally after 24 h of incubation of HSB.2 cells with 10(-8)-10(-6) M PGE2, sulprostone, M&B 28767, and misoprostol but not with 10(-6) M PGF2alpha, PGD2, PGI2, or butaprost, suggesting a principal dependence on EP3 Rs [6].
  • In the PT- and CT-treated cell membrane reconstituted with various G proteins, M&B 28767 inhibited the GTPase activity of G(o), but stimulated that of Gs [7].
  • The EP3-selective agonists, M&B 28,767 or GR 63799X, potently competed for the [3H]PGE2 binding, but no competition was found with EP1- or EP2-selective ligands [8].
  • PGE2 and M&B 28,767 decreased forskolin-induced cAMP formation in a concentration-dependent manner in Chinese hamster ovary cells permanently expressing the cDNA [8].

Biological context of Dpt-prostaglandin E1

  • The EP3-R agonist M&B28767 induced a time- and dose-dependent phosphorylation of the FLAG-rEP3hEP4-Ct-R but not of the FLAG-rEP3beta-R [9].
  • Transfection experiments revealed that all the four isoforms show high binding affinities to PGE2, PGE1, and M&B28767, an EP3-specific agonist, whereas their downstream signaling pathways are divergent [10].
  • To elucidate the possible mechanism of this desensitization, in vivo phosphorylation stimulated by activators of second messenger kinases, by prostaglandin E(2), or by the EP3-R agonist M&B28767 was investigated in COS-7 cells expressing FLAG-epitope-tagged rat EP3beta-R (rEP3beta-R), hEP4-R, or rEP3hEP4-Ct-R [9].
  • Both compounds given orally increased gastrointestinal motility in mice; M&B 28,767 (1-3 mg/kg) and DMPG (0.1-0.3 mg/kg) caused diarrhoea, the former being about 0.1 times as potent as the latter [4].
  • The remaining four analogs, 11-deoxy PGE2-1-alcohol, MB 28767, sulprostone, and GR 63779X did not induce vasodilatation and did not potentiate FMLP exudation [11].

Anatomical context of Dpt-prostaglandin E1


Associations of Dpt-prostaglandin E1 with other chemical compounds

  • The presence of the EP3 and EP4 Rs and the absence of the EP1 and EP2 Rs were revealed by inhibition of [3H]PGE2 binding by the EP3/EP1R agonist sulprostone, the EP3/EP2/EP4R agonist M&B 28767, and the EP2/EP4/EP3R agonist misoprostol but not by the EP1R antagonist SC-19220 or the EP2R agonist butaprost [13].
  • Thus, MB 28767, sulprostone and PGE2 were potent inhibitors, whereas PGF2 alpha, PGD2 and other analogs were substantially less potent [14].
  • The M&B 28767-stimulated GTPase activity consisted of pertussis-toxin-sensitive and cholera-toxin-sensitive portions in the EP3 gamma-expressing cell membrane, suggested that EP3 gamma is coupled to both guanine nucleotide-binding inhibitory and stimulatory proteins [15].

Gene context of Dpt-prostaglandin E1


  1. Prostaglandin E receptor EP3 subtype induces neurite retraction via small GTPase Rho. Katoh, H., Negishi, M., Ichikawa, A. J. Biol. Chem. (1996) [Pubmed]
  2. Prostaglandin E receptor EP3 subtype is involved in thermal hyperalgesia through its actions in the preoptic hypothalamus and the diagonal band of Broca in rats. Hosoi, M., Oka, T., Hori, T. Pain (1997) [Pubmed]
  3. Effects of the prostanoid EP3-receptor agonists M&B 28767 and GR 63799X on infarct size caused by regional myocardial ischaemia in the anaesthetized rat. Zacharowski, K., Olbrich, A., Otto, M., Hafner, G., Thiemermann, C. Br. J. Pharmacol. (1999) [Pubmed]
  4. M&B 28,767: a potent anti-secretory and anti-ulcer PG analogue. A comparative study with 16, 16' dimethyl PGE2 methylester. Banerjee, A.K., Christmas, A.J., Crowshaw, K., Heazell, M.A., Ivers-Read, G.C., Saunders, L.C., Wyatt, D. Life Sci. (1984) [Pubmed]
  5. Prostaglandin E(2) stimulates rat and human colonic mucin exocytosis via the EP(4) receptor. Belley, A., Chadee, K. Gastroenterology (1999) [Pubmed]
  6. Regulation of expression of matrix metalloproteinase-9 in early human T cells of the HSB.2 cultured line by the EP3 subtype of prostaglandin E2 receptor. Zeng, L., An, S., Goetzl, E.J. J. Biol. Chem. (1996) [Pubmed]
  7. Opposite coupling of prostaglandin E receptor EP3C with Gs and G(o). Stimulation of Gs and inhibition of G(o). Negishi, M., Namba, T., Sugimoto, Y., Irie, A., Katada, T., Narumiya, S., Ichikawa, A. J. Biol. Chem. (1993) [Pubmed]
  8. Cloning and expression of a cDNA for mouse prostaglandin E receptor EP3 subtype. Sugimoto, Y., Namba, T., Honda, A., Hayashi, Y., Negishi, M., Ichikawa, A., Narumiya, S. J. Biol. Chem. (1992) [Pubmed]
  9. Agonist-induced phosphorylation by G protein-coupled receptor kinases of the EP4 receptor carboxyl-terminal domain in an EP3/EP4 prostaglandin E(2) receptor hybrid. Neuschäfer-Rube, F., Oppermann, M., Möller, U., Böer, U., Püschel, G.P. Mol. Pharmacol. (1999) [Pubmed]
  10. Molecular cloning and expression of multiple isoforms of human prostaglandin E receptor EP3 subtype generated by alternative messenger RNA splicing: multiple second messenger systems and tissue-specific distributions. Kotani, M., Tanaka, I., Ogawa, Y., Usui, T., Mori, K., Ichikawa, A., Narumiya, S., Yoshimi, T., Nakao, K. Mol. Pharmacol. (1995) [Pubmed]
  11. Characterization of the EP-receptor mediating dilatation and potentiation of inflammation in rabbit skin. Armstrong, R.A., Marr, C., Jones, R.L. Prostaglandins (1995) [Pubmed]
  12. Molecular cloning and expression of a prostaglandin E2 receptor of the EP3 beta subtype from rat hepatocytes. Neuschäfer-Rube, F., DeVries, C., Hänecke, K., Jungermann, K., Püschel, G.P. FEBS Lett. (1994) [Pubmed]
  13. Selective regulation of RNK-16 cell matrix metalloproteinases by the EP4 subtype of prostaglandin E2 receptor. Zeng, L., An, S., Goetzl, E.J. Biochemistry (1996) [Pubmed]
  14. Radioligand binding analysis of receptor subtypes in two FP receptor preparations that exhibit different functional rank orders of potency in response to prostaglandins. Woodward, D.F., Fairbairn, C.E., Krauss, A.H., Lawrence, R.A., Protzman, C.E. J. Pharmacol. Exp. Ther. (1995) [Pubmed]
  15. Third isoform of the prostaglandin-E-receptor EP3 subtype with different C-terminal tail coupling to both stimulation and inhibition of adenylate cyclase. Irie, A., Sugimoto, Y., Namba, T., Harazono, A., Honda, A., Watabe, A., Negishi, M., Narumiya, S., Ichikawa, A. Eur. J. Biochem. (1993) [Pubmed]
  16. Multiple signal transduction pathways through two prostaglandin E receptor EP3 subtype isoforms expressed in human uterus. Kotani, M., Tanaka, I., Ogawa, Y., Suganami, T., Matsumoto, T., Muro, S., Yamamoto, Y., Sugawara, A., Yoshimasa, Y., Sagawa, N., Narumiya, S., Nakao, K. J. Clin. Endocrinol. Metab. (2000) [Pubmed]
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