Molecular Weight(MW): 415.57
Bimatoprost is a prostaglandin analog used topically (as eye drops) to control the progression of glaucoma and in the management of ocular hypertension.
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|Description||Bimatoprost is 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 [3H]prostaglandin F(2alpha) from FP receptors with K(i) of 6.31 μM. 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 μM and 2.2 μM.  Bimatoprost up-regulates Cyr61 mRNA expression in the cat iris. Bimatoprost-induced up-regulation of Cyr61 mRNA expression is not because of the activation of the prostaglandin FP receptor but a different receptor.  Bimatoprost consistently evokes responses in different cells within the same tissue preparation, whereas prostaglandin F(2 alpha) and 17-phenyl prostaglandin F(2 alpha) elicites signaling responses in the same cells. Bimatoprost selectively stimulates intracellular calcium signaling in different cat iris sphincter cells. 
|In vivo||Bimatoprost is the ethyl amide derivative of 17-phenyl trinor PGF2α, a potent prostaglandin FP receptor agonist. Bimatoprost elicits an immediate, robust spike in [Ca2+] that rapidly decayes back to baseline levels. Bimatoprost possess direct agonist activities at the rat, mouse, and human FP prostanoid receptor. |
-  Brubaker RF, et al. Surv Ophthalmol, 2001, 45 Suppl 4, S347-351.
-  Sharif NA, et al. Eur J Pharmacol, 2001, 432(2-3), 211-213.
-  Liang Y, et al. J Biol Chem, 2003, 278(29), 27267-27277.
|In vitro||Ethanol||83 mg/mL (199.72 mM)|
|DMSO||36 mg/mL (86.62 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02830776||Recruiting||Dermatochalasis||Tulane University|Allergan||November 2016||Early Phase 1|
|NCT02848300||Completed||Androgenetic Alopecia||Allergan||July 2016||Phase 1|
|NCT02863705||Recruiting||Glaucoma, Open-Angle|Normal Tension Glaucoma||Allergan||July 2016||Phase 4|
|NCT02676310||Recruiting||Alopecia|Alopecia, Androgenetic|Baldness||Allergan||March 2016||Phase 1|
|NCT02742649||Completed||Open-Angle Glaucoma|Ocular Hypertension||ForSight Vision5, Inc.||March 2016||Phase 1|Phase 2|
|NCT02636946||Recruiting||Glaucoma|Open-Angle Ocular Hypertension||Allergan||February 2016||Phase 3|
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