title: Design and synthesis of a highly selective EP2-receptor agonist.
abstract: EP2-receptor selective agonist 3 was identified by the structural hybridization of butaprost 1a and PGE(2) 2a. Based on this information, a chemically more stabilized 4 was discovered as another highly selective EP2-receptor agonist, iv administration of which to anesthetized rats suppressed uterine motility, while PGE(2) 2a stimulated uterine motility.
authors.affiliation: Minase Research Institute, Ono Pharmaceutical Co., Ltd., Shimamoto, Mishima, 618-8585, Osaka, Japan. k.tani@ono.co.jp
authors.forename: K
authors.initials: K
authors.lastname: Tani
authors.forename: A
authors.initials: A
authors.lastname: Naganawa
authors.forename: A
authors.initials: A
authors.lastname: Ishida
authors.forename: H
authors.initials: H
authors.lastname: Egashira
authors.forename: K
authors.initials: K
authors.lastname: Sagawa
authors.forename: H
authors.initials: H
authors.lastname: Harada
authors.forename: M
authors.initials: M
authors.lastname: Ogawa
authors.forename: T
authors.initials: T
authors.lastname: Maruyama
authors.forename: S
authors.initials: S
authors.lastname: Ohuchida
authors.forename: H
authors.initials: H
authors.lastname: Nakai
authors.forename: K
authors.initials: K
authors.lastname: Kondo
authors.forename: M
authors.initials: M
authors.lastname: Toda
mesh_terms: D000527:Alprostadil / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D000818:Animals; D001665:Binding Sites / Q000502:physiology; D016466:CHO Cells / Q000378:metabolism; D006224:Cricetinae; D000242:Cyclic AMP / Q000819:agonists; D003503:Cyclobutanes / Q000138:chemical synthesis* / Q000494:pharmacology*; D003517:Cyclopentanes / Q000138:chemical synthesis* / Q000494:pharmacology*; D015232:Dinoprostone / Q000378:metabolism / Q000494:pharmacology; D015195:Drug Design; D005260:Female; D006801:Humans; D008024:Ligands; D051379:Mice; D051381:Rats; D018078:Receptors, Prostaglandin E / Q000819:agonists*; D058307:Receptors, Prostaglandin E, EP2 Subtype; D012680:Sensitivity and Specificity; D014590:Uterine Contraction / Q000187:drug effects*
chemical_list: D003503:Cyclobutanes; D003517:Cyclopentanes; D008024:Ligands; C545644:PTGER2 protein, human; C545645:Ptger2 protein, mouse; D018078:Receptors, Prostaglandin E; D058307:Receptors, Prostaglandin E, EP2 Subtype; D000242:Cyclic AMP; D000527:Alprostadil; C048491:butaprost; D015232:Dinoprostone