Design and synthesis of a highly selective EP2-receptor agonist

Bioorg Med Chem Lett. 2001 Aug 6;11(15):2025-8. doi: 10.1016/s0960-894x(01)00359-6.

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.

MeSH terms

  • Alprostadil / analogs & derivatives*
  • Alprostadil / chemical synthesis
  • Animals
  • Binding Sites / physiology
  • CHO Cells / metabolism
  • Cricetinae
  • Cyclic AMP / agonists
  • Cyclobutanes / chemical synthesis*
  • Cyclobutanes / pharmacology*
  • Cyclopentanes / chemical synthesis*
  • Cyclopentanes / pharmacology*
  • Dinoprostone / metabolism
  • Dinoprostone / pharmacology
  • Drug Design
  • Female
  • Humans
  • Ligands
  • Mice
  • Rats
  • Receptors, Prostaglandin E / agonists*
  • Receptors, Prostaglandin E, EP2 Subtype
  • Sensitivity and Specificity
  • Uterine Contraction / drug effects*

Substances

  • Cyclobutanes
  • Cyclopentanes
  • Ligands
  • PTGER2 protein, human
  • Ptger2 protein, mouse
  • Receptors, Prostaglandin E
  • Receptors, Prostaglandin E, EP2 Subtype
  • Cyclic AMP
  • Alprostadil
  • butaprost
  • Dinoprostone