| Description | Bimatoprost (AGN 192024) is a cloprostenol-derived amide that is used as an antihypertensive agent in the treatment of open-angle glaucoma and ocular hypertension. |
| In vitro | Bimatoprost是有效的前列腺素FP受体激动剂.其可直接使强有力的钙离子快速回到基线水平.Bimatoprost可直接激动大鼠,小鼠及人类的FP前列腺素受体. |
| In vivo | Bimatoprost置换[3H]前列腺素F（2alpha）结合FP受体（Ki：6.31 μM）。在表达FP受体的3T3小鼠成纤维细胞（EC50：2.2 μM）（EC50：2.94 μM）和人FP受体的人类胚胎肾细胞中,Bimatoprost可使细胞内钙离子迅速动员。 Bimatoprost对猫虹膜中的Cyr61表达具有上调效果。Bimatopros对房水的流动速率有轻度刺激效果,白天为13％,夜间为14％,向外流的tonographic性降低26％,从而使眼压降低。 |
| Synonyms | AGN 192024, 比马前列素 |
| molecular weight | 415.57 |
| Molecular formula | C25H37NO4 |
| CAS | 155206-00-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 34 mg/mL (81.8 mM) Ethanol: 77 mg/mL (185.3 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) |
| References | 1. Brubaker RF, et al. Surv Ophthalmol, 2001, 45 Suppl 4, S347-351. 2. Sharif NA, et al. Eur J Pharmacol, 2001, 432(2-3), 211-213. 3. Liang Y, et al. J Biol Chem, 2003, 278(29), 27267-27277. 4. Spada CS, et al. Exp Eye Res, 2005, 80(1), 135-145. 5. Kelly CR, et al. J Pharmacol Exp Ther, 2003, 304(1), 238-245. |