Design and Synthesis of a Highly Selective EP2-Receptor Agonist

Design and Synthesis of a Highly Selective EP2-Receptor Agonist

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...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2001-08, Vol.11 (15), p.2025-2028
Hauptverfasser: Tani, Kousuke, Naganawa, Atsushi, Ishida, Akiharu, Egashira, Hiromu, Sagawa, Kenji, Harada, Hiroyuki, Ogawa, Mikio, Maruyama, Takayuki, Ohuchida, Shuichi, Nakai, Hisao, Kondo, Kigen, Toda, Masaaki
Format: Artikel
Sprache:eng
Schlagworte:
Alprostadil - analogs & derivatives
Alprostadil - chemical synthesis
Animals
Binding Sites - physiology
Biological and medical sciences
CHO Cells - metabolism
Cricetinae
Cyclic AMP - agonists
Cyclobutanes - chemical synthesis
Cyclobutanes - pharmacology
Cyclopentanes - chemical synthesis
Cyclopentanes - pharmacology
Dinoprostone - metabolism
Dinoprostone - pharmacology
Drug Design
Female
Genital system. Reproduction
Humans
Ligands
Medical sciences
Mice
Pharmacology. Drug treatments
Rats
Receptors, Prostaglandin E - agonists
Receptors, Prostaglandin E, EP2 Subtype
Sensitivity and Specificity
Uterine Contraction - drug effects
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Zusammenfassung: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. A highly selective EP2-receptor agonist 4, which is able to be used for in vivo studies, was identified.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(01)00359-6