高选择性EP2受体激动剂的设计与合成
Design and synthesis of a highly selective EP2-receptor agonist.
作者信息
Tani K, Naganawa A, Ishida A, Egashira H, Sagawa K, Harada H, Ogawa M, Maruyama T, Ohuchida S, Nakai H, Kondo K, Toda M
机构信息
Minase Research Institute, Ono Pharmaceutical Co., Ltd., Shimamoto, Mishima, 618-8585, Osaka, Japan.
出版信息
Bioorg Med Chem Lett. 2001 Aug 6;11(15):2025-8. doi: 10.1016/s0960-894x(01)00359-6.
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.
EP2 受体选择性激动剂 3 是通过布他前列素 1a 与前列腺素 E2（PGE2）2a 的结构杂交鉴定出来的。基于这一信息，发现了一种化学性质更稳定的化合物 4，它是另一种高度选择性的 EP2 受体激动剂，对麻醉大鼠静脉注射该化合物可抑制子宫运动，而 PGE2 2a 则刺激子宫运动。
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