Quantitative Autoradiographic Visualization and Pharmacology of FP-Prostaglandin Receptors in Human Eyes Using the Novel Phosphor-Imaging Technology

Davis, T. W.; Sharif, Naj

doi:10.1089/jop.1999.15.323

Cited by 52 publications

(42 citation statements)

References 18 publications

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“…The exact cellular and molecular mechanism of action of these FP prostaglandin agonists is not known, although some evidence exists implicating the release of matrix metalloproteinases (MMPs) resulting in the digestion of the extracellular matrix accumulated in the uveoscleral tract and perhaps also in the structures linked to the conventional outflow pathway (14,15,(16)(17)(18). Although the presence of FP receptor mRNA (19,22) and FP receptor-induced relaxation of cynomolgus monkey ciliary muscle were reported (20), and FP receptors have been autoradiographically (2,21) and immunohistochemically (19,22) visualized on human ciliary muscles, the detailed pharmacological characterization of these FP receptors and their signal transduction pathways have not yet been investigated in isolated human ciliary muscle (h-CM) cells.…”

Section: Introductionmentioning

confidence: 99%

Human Ciliary Muscle Cell Responses to FP-Class Prostaglandin Analogs: Phosphoinositide Hydrolysis, Intracellular Ca²⁺ Mobilization and MAP Kinase Activation

Sharif

Crider

Husain

et al. 2003

Journal of Ocular Pharmacology and Therapeutics

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Phospholipase C induced phosphoinositide (PI) turnover, intracellular Ca(2+) ([Ca(2+)](i)) mobilization and mitogen-activated protein (MAP) kinase activation by FP-class prostaglandin analogs was studied in normal human ciliary muscle (h-CM) cells. Agonist potencies obtained in the PI turnover assays were: travoprost acid ((+)-fluprostenol; EC(50) = 2.6 +/- 0.8 nM) > bimatoprost acid (EC(50) = 3.6 +/- 1.2 nM) > (+/-)-fluprostenol (EC(50) = 4.3 +/- 1.3 nM) >> prostaglandin F(2 alpha) (PGF(2 alpha)) (EC(50) = 134 +/- 17 nM) > latanoprost acid (EC(50) = 198 +/- 83 nM) > S-1033 (EC(50) = 2930 +/- 1420 nM) > unoprostone (EC(50) = 5590 +/- 1490 nM) > bimatoprost (EC(50) = 9600 +/- 1100 nM). Agonist potencies in h-CM cells correlated well with those previously obtained for the cloned human ciliary body-derived FP receptor (r = 0.96, p< 0.001) and that present on h-TM cells (r = 0.94, p< 0.0001). Travoprost acid, PGF(2 alpha) and unoprostone also stimulated [Ca(2+)](i) mobilization in h-CM cells with travoprost acid being the most potent agonist. MAP kinase activity was stimulated in the h-CM cells with the following rank order of activity (at 100 nM): travoprost acid > PGF(2 alpha) > latanoprost acid > PGD(2) > bimatoprost > latanoprost = bimatoprost acid = fluprostenol > PGE(2) = S-1033 > unoprostone > PGI(2). The PI turnover, [Ca(2+)](i) mobilization and MAP kinase activation induced by several of these agonists was blocked by the FP receptor antagonist, AL-8810 (11 beta-fluoro-15-epiindanyl PGF(2 alpha)) (e.g. K(i) = 5.7 microM versus PI turnover). These studies have characterized the biochemical and pharmacological properties of the native FP prostaglandin receptor present on h-CM cells using three signal transduction mechanism assays and a broad panel of FP-class agonist analogs (including free acids of bimatoprost, travoprost and latanoprost) and the FP receptor antagonist, AL-8810.

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Section: Introductionmentioning

confidence: 99%

Human Ciliary Muscle Cell Responses to FP-Class Prostaglandin Analogs: Phosphoinositide Hydrolysis, Intracellular Ca²⁺ Mobilization and MAP Kinase Activation

Sharif

Crider

Husain

et al. 2003

Journal of Ocular Pharmacology and Therapeutics

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“…Tafluprost has a 12-times higher affinity than latanoprost for prostanoid FP receptor (FP) [21], which have been known to be expressed in the ganglion cells [6,17]. This difference suggested tafluprost has the protective effect via other receptors.…”

Section: Discussionmentioning

confidence: 99%

Tafluprost protects rat retinal ganglion cells from apoptosis in vitro and in vivo

Kanamori

Naka

Fukuda

et al. 2009

Graefes Arch Clin Exp Ophthalmol

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“…Travoprost acid has greater affinity for prostaglandin F receptor than either prostaglandin F 2a or latanoprost acid. 8,20 The receptors are abundant in the longitudinal ciliary muscle of the human eye and iris sphincter. 20 The IOP-lowering efficacy of travoprost was found to be comparable to latanoprost and timoptic.…”

Section: Discussionmentioning

confidence: 99%

“…8,20 The receptors are abundant in the longitudinal ciliary muscle of the human eye and iris sphincter. 20 The IOP-lowering efficacy of travoprost was found to be comparable to latanoprost and timoptic. 8 Although orally administered carbonic anhydrase inhibitors suppress aqueous humour production by 20À35%, they are associated with significant side effects.…”

Section: Discussionmentioning

confidence: 99%

Comparing the effects of travoprost and brinzolamide on intraocular pressure after phacoemulsification

Ermiş

Öztürk

İnan

2004

Eye

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Purpose To evaluate the intraocular pressure (IOP) lowering effect of travoprost and brinzolamide within the first 24 h after phacoemulsification cataract surgery. Methods This prospective, randomized, double-masked, controlled study comprised 90 eyes of 90 consecutive patients with senile cataract who had uneventful phacoemulsification surgery. Eyes in the first group received travoprost 0.0015%, second group received brinzolamide 1%. Eyes in the third group received balanced salt solution and were used as control. One drop was instilled immediately after surgery. IOP was measured 24 h preoperatively, 6 and 24 h postoperatively. Analysis of variance, Student's-t and w 2 -tests were used for statistical analyses. Results Preoperatively IOP was not significantly different among the three groups (P ¼ 0.653). At 6 and 24 h postoperatively IOP was lower in both travoprost and brinzolamide group when compared to control group (P ¼ 0.018 and 0.015 at 6 h, P ¼ 0.010 and 0.012 at 24 h, respectively). The difference between travoprost and brinzolamide group was not significant (P ¼ 0.859 at 6 h and P ¼ 0.581 at 24 h). Both travoprost and brinzolamide significantly reduced IOP increases when compared to control eyes at 6 and 24 h (P ¼ 0.036 and 0.029 at 6 h, P ¼ 0.010 and 0.007 at 24 h, respectively). The difference in IOP increase at 6 and 24 h between travoprost and brinzolamide group was not significant (P ¼ 0.744 at 6 h and P ¼ 0.672 at 24 h). Conclusion Both travoprost and brinzolamide significantly lowered IOP after small incision phacoemulsification cataract surgery within the first 24 h without any side effect.

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Quantitative Autoradiographic Visualization and Pharmacology of FP-Prostaglandin Receptors in Human Eyes Using the Novel Phosphor-Imaging Technology

Cited by 52 publications

References 18 publications

Human Ciliary Muscle Cell Responses to FP-Class Prostaglandin Analogs: Phosphoinositide Hydrolysis, Intracellular Ca²⁺ Mobilization and MAP Kinase Activation

Human Ciliary Muscle Cell Responses to FP-Class Prostaglandin Analogs: Phosphoinositide Hydrolysis, Intracellular Ca²⁺ Mobilization and MAP Kinase Activation

Tafluprost protects rat retinal ganglion cells from apoptosis in vitro and in vivo

Comparing the effects of travoprost and brinzolamide on intraocular pressure after phacoemulsification

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Quantitative Autoradiographic Visualization and Pharmacology of FP-Prostaglandin Receptors in Human Eyes Using the Novel Phosphor-Imaging Technology

Cited by 52 publications

References 18 publications

Human Ciliary Muscle Cell Responses to FP-Class Prostaglandin Analogs: Phosphoinositide Hydrolysis, Intracellular Ca2+ Mobilization and MAP Kinase Activation

Human Ciliary Muscle Cell Responses to FP-Class Prostaglandin Analogs: Phosphoinositide Hydrolysis, Intracellular Ca2+ Mobilization and MAP Kinase Activation

Tafluprost protects rat retinal ganglion cells from apoptosis in vitro and in vivo

Comparing the effects of travoprost and brinzolamide on intraocular pressure after phacoemulsification

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Human Ciliary Muscle Cell Responses to FP-Class Prostaglandin Analogs: Phosphoinositide Hydrolysis, Intracellular Ca²⁺ Mobilization and MAP Kinase Activation

Human Ciliary Muscle Cell Responses to FP-Class Prostaglandin Analogs: Phosphoinositide Hydrolysis, Intracellular Ca²⁺ Mobilization and MAP Kinase Activation