AL 8810 is an 11β-fluoro analog of PGF2α which acts as a potent and selective antagonist at the PGF2αR (FP receptor). AL 8810 has weak intrinsic agonist activity on FP receptor preparations in the 200-300 nM range, yet it fully antagonizes the activity of the potent FP receptor agonist fluprostenol at this concentration, with EC50 values of approximately 430 nM. AL 8810 fully antagonized the bimatoprost-induced calcium mobilization in Swiss 3T3 fibroblasts at 100 μM, indicating that bimatoprost acts as an FP agonist in this preparation. The Ki for the inhibition of several potent agonists at the cloned human ciliary body FP receptor is in the range of 1-2 μM.
1 Griffen, B.W., Klimko, P., Crider, J.Y., et al. AL-8810: A novel prostaglandin F2α analog with selective antagonist effects at the prostaglandin F2α (FP) receptor. J Pharmacol Exp Ther 290 1278-1284 (1999). 2 Sharif, N.A., Williams, G.W., Kelly, C.R. Bimatoprost and its free acid are prostaglandin FP receptor agonists. Eur J Pharmacol 432 211-213 (2001). 3 Sharif, N.A., Kelly, C.R., Crider, J.Y. Agonist activity of Bimatoprost, Travoprost, Latanoprost, Unoprostone isopropyl ester and other prostaglandin analogs at the cloned human ciliary body FP prostaglandin receptor. J Ocul Pharmacol 18 313-324 (2002 Feb 27).
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