比马前列素及其游离酸是前列腺素FP受体激动剂。
Bimatoprost and its free acid are prostaglandin FP receptor agonists.
作者信息
Sharif N A, Williams G W, Kelly C R
机构信息
Molecular Pharmacology Unit, Alcon Research, Ltd., 6201 South Freeway, Fort Worth, TX 76134, USA.
出版信息
Eur J Pharmacol. 2001 Dec 7;432(2-3):211-3. doi: 10.1016/s0014-2999(01)01486-8.
Bimatoprost (17-phenyl-prostaglandin F(2alpha) ethyl amide) has been reported not to exert its actions via prostaglandin receptors. Here, bimatoprost displaced [3H]prostaglandin F(2alpha) from FP receptors (K(i)=6310+/-1650 nM). Bimatoprost rapidly mobilized intracellular Ca(2+) (Ca(2+)) via cloned human FP receptors expressed in human embryonic kidney cells (EC(50)=2940+/-1663 nM) and via native FP receptors in 3T3 mouse fibroblasts (EC(50)=2200+/-670 nM). Furthermore, AL-8810 ((5Z, 13E)-(9S,11S,15R)-9,15-dihydroxy-11-fluoro-15-(2-indanyl)-16,17,18,19,20-pentanor-5,13-prostadienoic acid), an FP receptor antagonist, blocked the bimatoprost-induced Ca(2+) mobilization.
比马前列素（17-苯基-前列腺素F(2α) 乙酰胺）据报道并非通过前列腺素受体发挥作用。在此，比马前列素从FP受体上取代了[3H]前列腺素F(2α)（抑制常数K(i)=6310±1650纳摩尔）。比马前列素通过在人胚肾细胞中表达的克隆人FP受体（半数有效浓度EC(50)=2940±1663纳摩尔）以及通过3T3小鼠成纤维细胞中的天然FP受体快速动员细胞内钙离子（[Ca(2+)]i）（半数有效浓度EC(50)=2200±670纳摩尔）。此外，FP受体拮抗剂AL-8810（(5Z, 13E)-(9S,11S,15R)-9,15-二羟基-11-氟-15-(2-茚满基)-16,17,18,19,20-五降-5,13-前列腺二烯酸）阻断了比马前列素诱导的[Ca(2+)]i动员。
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