比马前列素（卢美根（商标名））是克隆的人眼FP前列腺素受体的激动剂：基于荧光成像板读数器的实时细胞内钙离子动员研究。
Bimatoprost (Lumigan((R))) is an agonist at the cloned human ocular FP prostaglandin receptor: real-time FLIPR-based intracellular Ca(2+) mobilization studies.
作者信息
Sharif N A, Kelly C R, Williams G W
机构信息
Molecular Pharmacology Unit (R2-19), Alcon Research Limited, 6201 South Freeway, 76134, Fort Worth, TX, USA.
出版信息
Prostaglandins Leukot Essent Fatty Acids. 2003 Jan;68(1):27-33. doi: 10.1016/s0952-3278(02)00232-6.
Bimatoprost is the ethyl amide derivative of 17-phenyl-trinor prostaglandin F(2alpha). Here, we show that bimatoprost (K(i)=9250+/-846nM) and bimatoprost free acid (17-phenyl-trinor prostaglandin F(2alpha); K(i)=59+/-6nM) bind to the FP receptor and displace [(3)H]-travoprost acid, a selective FP agonist. Bimatoprost (EC(50)=3070+/-1330nM), Lumigan((R)) (bimatoprost 0.03% ophthalmic solution; EC(50)=1150+/-93nM) and bimatoprost acid (EC(50)=15+/-3nM) mobilized intracellular Ca(2+) (Ca(2+)) in <5s in HEK-293 cells expressing the cloned human ciliary body FP receptor on a fluorometric imaging plate reader (FLIPR). Furthermore, agonist effects of bimatoprost and bimatoprost acid were blocked by AL-8810 (11beta-fluoro-15-epi-15-indanyl prostaglandin F(2alpha); K(i)=0.7-2.1 MicroM), an FP receptor-selective antagonist. Therefore, the prodrug bimatoprost and its hydrolytic product, bimatoprost free acid, bind to and activate the human ocular FP prostaglandin receptor to mobilize Ca(2+), thus behaving as FP receptor agonists.
比马前列素是17 - 苯基 - 三降前列腺素F(2α)的乙酰胺衍生物。在此，我们表明比马前列素（K(i)=9250±846 nM）和比马前列素游离酸（17 - 苯基 - 三降前列腺素F(2α)；K(i)=59±6 nM）与FP受体结合，并取代[(3)H] - 曲伏前列酸（一种选择性FP激动剂）。比马前列素（EC(50)=3070±1330 nM）、卢美根（Lumigan((R))，比马前列素0.03%眼用溶液；EC(50)=1150±93 nM）和比马前列酸（EC(50)=15±3 nM）在荧光成像板读数器（FLIPR）上，能在<5秒内使表达克隆人睫状体FP受体的HEK - 293细胞内的钙离子（Ca(2+)）动员起来。此外，比马前列素和比马前列酸的激动作用被FP受体选择性拮抗剂AL - 8810（11β - 氟 - 15 - 表 - 15 - 茚满基前列腺素F(2α)；K(i)=0.7 - 2.1 μM）所阻断。因此，前药比马前列素及其水解产物比马前列素游离酸与人类眼部FP前列腺素受体结合并激活该受体，从而动员Ca(2+)，表现为FP受体激动剂。
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