Bimatoprost (AGN 192024)

Description: Bimatoprost (AGN 192024) is a potent FP receptor agonist and a prostaglandin analog used topically as eye drops to control the progression of glaucoma and in the management of ocular hypertension. Bimatoprost mildly stimulates the rate of aqueous humor flow during the day (13%) and at night (14%), its ocular hypotensive action is due primarily to a 26% reduction in the tonographic resistance to outflow. Bimatoprost enhances the pressure-sensitive outflow pathway. Bimatoprost displaces 3Hprostaglandin F(2alpha) from FP receptors with K(i) of 6.31 uM. Bimatoprost rapidly mobilizes intracellular Ca(2+) via cloned human FP receptors expressed in human embryonic kidney cells and via native FP receptors in 3T3 mouse fibroblasts with EC(50) of 2.94 uM and 2.2 uM.

References: Surv Ophthalmol. 2001 May; 45 Suppl 4:S347-51; Eur J Pharmacol. 2001 Dec 7; 432(2-3):211-3; J Pharmacol Exp Ther. 2003 Jan; 304(1):238-45.