Identification and pharmacological characterization of the prostaglandin FP receptor and FP receptor variant complexes

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Identification and pharmacological characterization of the prostaglandin FP receptor and FP receptor variant complexes

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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Colocalization of prostaglandin F(2alpha) receptor FP and prostaglandin F synthase-I in the spinal cord.

Prostaglandin F(2alpha) is synthesized by prostaglandin F synthase, which exists in two types, prostaglandin F synthase I (PGFS I) and prostaglandin F synthase II (PGFS II). Prostaglandin F(2alpha) binds to its specific receptor, FP. Our previous immunohistochemical study showed the distinct localization of prostaglandin F synthases in rat spinal cord. PGFS I exists in neuronal somata and dendr...

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The effects of prostaglandin analogues on IOP in prostanoid FP-receptor-deficient mice.

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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Effect of latanoprost on intraocular pressure in mice lacking the prostaglandin FP receptor.

PURPOSE To determine whether latanoprost lowers IOP in prostaglandin FP receptor knockout mice. METHODS Mean IOP difference between treated and untreated fellow eyes was measured on three separate occasions, 2 hours after a 200-ng dose of latanoprost to the right eye of homozygous (n = 9) and heterozygous (n = 15) FP knockout mice. C57BL/6 (n = 10) and NIH Swiss white mice (n = 17), which hav...

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Pharmacological characterization of an FP prostaglandin receptor on rat vascular smooth muscle cells (A7r5) coupled to phosphoinositide turnover and intracellular calcium mobilization.

An FP prostaglandin (PG) receptor on the A7r5 rat aorta smooth muscle cell line has been characterized by assays of phosphoinositide (PI) turnover and intracellular calcium mobilization stimulated by structurally diverse PGs. In the PI turnover assay, cloprostenol was the most potent PG tested, with a potency (EC50) of 0.84 +/- 0.06 nM (mean +/- S.E.M., n = 34), and was a full agonist. Other kn...

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ژورنال

عنوان ژورنال: British Journal of Pharmacology

سال: 2008

ISSN: 0007-1188

DOI: 10.1038/bjp.2008.142