Corpus ID: 21272423

EP3, but not EP2, FP, or TP prostanoid-receptor stimulation may reduce intraocular pressure.

@article{Waterbury1990EP3BN,
  title={EP3, but not EP2, FP, or TP prostanoid-receptor stimulation may reduce intraocular pressure.},
  author={L. David Waterbury and R. M. Eglen and G F Faurot and GRAHAME F. Cooper},
  journal={Investigative ophthalmology \& visual science},
  year={1990},
  volume={31 12},
  pages={
          2560-7
        }
}
Stimulation of DP, but not TP or FP, prostanoid receptors has previously been shown to reduce intraocular pressure (IOP) in rabbits. However the role of EP receptors (EP1, EP2, and EP3 subtypes) has not been studied extensively. Sulprostone, RS-61565, and RS-20216 have been studied for effects on rabbit IOP, and their prostanoid-receptor profiles characterized. The data suggest that the EP3, but not EP2, FP, or TP activity of these agonists correlated with the intraocular hypotensive effects… 
The effects of prostaglandin analogues on prostanoid EP1, EP2, and EP3 receptor-deficient mice.
TLDR
Deficiency of EP receptors had no effect on physiological IOP, and EP1 and EP2 receptors are not involved in prostaglandin analogue-induced IOP reduction, whereas EP3 receptors may play a role.
Further studies on ocular responses to DP receptor stimulation.
TLDR
Findings reinforce the concept that selective DP receptor agonists may be useful for lowering intraocular pressure without causing ocular surface pathology and suggest a possible subdivision of the DP receptor designation.
Responses of intraocular pressure and the pupil of feline eyes to prostaglandin EP1 and FP receptor agonists.
TLDR
In cats, intraocular pressure and pupil responses to PGF2alpha, are mediated by EP1 and FP receptors, respectively; however, SC19220 significantly and dose-dependently inhibited the pupil response to 17-phenyl trinor PGE2alpha suggesting that EP1 receptors mediate pupils response to this agonist.
IOP-Lowering Effect of ONO-9054, A Novel Dual Agonist of Prostanoid EP3 and FP Receptors, in Monkeys.
TLDR
A more profound and longer-lasting reduction in IOP in normotensive monkeys can be observed with ONO-9054, which simultaneously stimulates both EP3 and FP receptors, compared with prostaglandin analogs.
Prostanoid EP1‐ and TP‐receptors involved in the contraction of human pulmonary veins
TLDR
The results indicate that FP‐receptors are not implicated in the contraction of human pulmonary veins and suggest that the contractions induced by prostanoids involved TP‐ and EP1‐ receptors in human pulmonary venous smooth muscle.
The EP2 receptor is the predominant prostanoid receptor in the human ciliary muscle.
TLDR
The results indicate that the dominant prostanoid receptor in the human ciliary muscle is the EP2 subclass and that there is also a small number of DP receptors.
The role of the prostaglandin EP4 receptor in the regulation of human outflow facility.
TLDR
Activation of PG-EP(4) receptors expressed by SC cells of the human conventional outflow pathway appears to contribute to PG regulation of outflow facility.
The IOP-lowering effects and mechanism of action of tafluprost in prostanoid receptor-deficient mice
TLDR
It is concluded that a part of ocular hypotensive effect of tafluprost is attributed to FP receptor-mediated prostaglandin production acting through the prostanoid EP3 receptor.
Initial clinical studies with prostaglandins and their analogues.
TLDR
17-phenyl substituted PGF2 alpha-IE analogues, such as PhXA34 or latanoprost, effectively reduce IOP by 30-40% for at least 24 hours, and are very well tolerated with minimal conjunctival hyperemia and without irritation.
Prostaglandins in the eye: Function, expression, and roles in glaucoma
TLDR
The modes of action of each of the prostaglandin molecules, their expression, their role in aqueous humour production and outflow within the eye, as well as their roles as medications for the treatment of glaucoma are examined.
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References

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The action of prostanoid receptor agonists and antagonists on smooth muscle and platelets
TLDR
Prostanoid receptors have been characterized in a range of guinea‐pig and rat smooth muscle and platelets using agonists and putative selective antagonists, and misoprostol and fenprostalene were characterized using the above preparations.
Studies on the ocular pharmacology of prostaglandin D2.
TLDR
Both the ocular hypotensive actions and the conjunctival pathology of PGD2 may be replicated individually by employing PGD1 analogues and metabolites by employing selective DP-receptor agonists.
Effects of prostaglandin D2 and its analogues on intraocular pressure in rabbits.
TLDR
PGE2 was the strongest in causing these side effects, followed by PGF2 alpha, and PGD2 did not cause any of these responses except for some development of conjunctival hyperemia.
Prostaglandin F2 alpha effects on intraocular pressure negatively correlate with FP-receptor stimulation.
TLDR
The intraocular pressure response to PGF2 alpha and selected analogues was compared with their rank order of activity in typical FP-receptor preparations such as contraction of the cat iris sphincter and affinity for corporal luteal membrane binding sites and it was concluded that the ocular hypotensive effect of P GF2 alpha is not mediated by the FP- receptor.
Iloprost, a stable prostacyclin analog, reduces intraocular pressure.
TLDR
It is suggested that similar low doses of an analog of Iloprost or carboprostacyclin that does not affect the hemodynamic equilibrium could be of value in the treatment of glaucoma.
Comparison of the ocular hypotensive efficacy of eicosanoids and related compounds.
  • L. Bito
  • Medicine
    Experimental eye research
  • 1984
TLDR
The ocular hypotensive efficacy and some of the ocular side-effects of 15 eicosanoids and related compounds, especially derivatives of PGF2 alpha, were compared and were also compared to some clinically used ocular hypertensive agents.
The effect of intravitreal and topical prostaglandins on intraocular inflammation.
TLDR
The classic signs of intraocular inflammation, i.e., increase in IOP, increase in protein content of the aQueous, miosis, and PMN entry into aqueous, are not necessarily associated and sequential, and PGs do not induce all signs of inflammation.
COMPARISON OF THE ACTIONS OF U‐46619, A PROSTAGLANDIN H2‐ANALOGUE, WITH THOSE OF PROSTAGLANDIN H2 AND THROMBOXANE A2 ON SOME ISOLATED SMOOTH MUSCLE PREPARATIONS
TLDR
It is suggested that U‐46619 is a selective TxA2‐mimetic and that it should therefore be a valuable tool in the study of the actions of TXA2.
Eicosanoids as a new class of ocular hypotensive agents. 1. The apparent therapeutic advantages of derived prostaglandins of the A and B type as compared with primary prostaglandins of the E, F and D type.
TLDR
Findings suggest that derived PGs, especially PGs of the A type, may have a therapeutic advantage over primary PGs for the treatment of ocular hypertension and glaucoma.
Characterization of the prostanoid receptor profile of enprostil and isomers in smooth muscle and platelets in vitro
TLDR
Enprostil and the ‘natural’ R and S isomers, therefore, were EP3, FP and TP agonists, being most potent at the EP3 receptor.
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