Real-Time Intracellular Ca Mobilization by Travoprost Acid, Bimatoprost, Unoprostone, and Other Analogs via Endogenous Mouse, Rat, and Cloned Human FP Prostaglandin Receptors
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چکیده
The ability of a number of prostaglandin F2 (PGF2 ) analogs to mobilize intracellular Ca [Ca ]i and to compete for [H]PGF2 binding to prostaglandin F2 receptors (FP) was evaluated. Radioligand binding studies measuring displacement of [H]PGF2 by a variety of FP prostaglandin analogs yielded the following rank order of affinities: travoprost acid [( )-16-m-trifluorophenoxy tetranor PGF2 ; ( )-fluprostenol] bimatoprost acid (17-phenyl-trinor PGF2 ) unoprostone (13,14-dihydro-15-keto-20-ethyl PGF2 ) bimatoprost (17phenyl-trinor PGF2 ethyl amide) Lumigan (bimatoprost ophthalmic solution). In FP functional studies, travoprost acid (EC50 17.5–37 nM, n 13), bimatoprost acid (EC50 23.3– 49.0 nM, n 6–12), unoprostone (EC50 306-1270 nM, n 4–8), bimatoprost (EC50 30703940 nM, n 4–9), and Lumigan (EC5
منابع مشابه
Real-time intracellular Ca2+ mobilization by travoprost acid, bimatoprost, unoprostone, and other analogs via endogenous mouse, rat, and cloned human FP prostaglandin receptors.
The ability of a number of prostaglandin F 2 alpha (PGF 2 alpha) analogs to mobilize intracellular Ca2+[Ca2+]iand to compete for [3H]PGF 2 alpha binding to prostaglandin F 2 alpha receptors (FP) was evaluated. Radioligand binding studies measuring displacement of [3H]PGF 2 alpha by a variety of FP prostaglandin analogs yielded the following rank order of affinities: travoprost acid [(+)-16-m-tr...
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The prostaglandin analogs have emerged as effective, well-tolerated agents for the reduction of intraocular pressure (IOP) in patients with primary open-angle glaucoma and ocular hypertension. Based on the available clinical data, bimatoprost, latanoprost and travoprost appear to be at more effective than the erstwhile gold standard, timolol, while the effectiveness of unoprostone is similar or...
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PURPOSE This study was designed to clarify the involvement of the prostanoid FP receptor in the intraocular pressure (IOP)-lowering effects of latanoprost, travoprost, bimatoprost, and unoprostone with the use of FP-receptor-deficient (FPKO) mice. METHODS FPKO and wild-type (WT) mice were bred and acclimatized under a 12-hour light-dark cycle. IOP was measured under general anesthesia by a mi...
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BACKGROUND AND PURPOSE A prostamide analogue, bimatoprost, has been shown to be effective in reducing intraocular pressure, but its precise mechanism of action remains unclear. Hence, to elucidate the molecular mechanisms of this effect of bimatoprost, we focused on pharmacologically characterizing prostaglandin FP receptor (FP) and FP receptor variant (altFP) complexes. EXPERIMENTAL APPROACH...
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