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Chemical Compound Review:

AC1NSK7N 2-[(Z)-4-[(1R,2S,3R,5R)-5- chloro-3-hydroxy...

Synonyms: ZK118182

Sharif, N.A. et al., Davis, T.L. et al., Sharif, N.A. et al.

Sharif, Williams, Crider, Xu, Davis, Sharif, Crider, Xu, Williams,

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Disease relevance of ZK118182

DP-class prostaglandins and prostaglandin analogs (collectively, prostaglandins or PGs) such as PGD2, BW245C, ZK110841, and ZK118182, lower intraocular pressure (IOP) in animal models of ocular hypertension [1].

High impact information on ZK118182

Interestingly, synthetic DP receptor-specific agonists such as BW245C (K(i)=64.7+/-1.0 nM; n=3) and ZK118182 (K(i)=425+/-42 nM; n=4), and the purported EP(3) receptor-specific ligand enprostil (K(i)=43.1+/-4.4 nM), also displayed high affinity for the EP(4) receptor [2].
ZK110841 and ZK118182 exhibited a relatively high potency at the adenylyl cyclase-coupled EP(2) receptor in human nonpigmented ciliary epithelial cells but were partial agonists [3].
DP receptor agonists produced cAMP in embryonic bovine tracheal fibroblasts with different potencies (EC(50) values in nM): ZK118182 (18 +/- 6), RS93520 (28 +/- 6), SQ27986 (29 +/- 7), ZK110841 (31 +/- 7), BW245C (53 +/- 16), and PGD(2) (98 +/- 10) [3].

References

Molecular pharmacology of the DP/EP2 class prostaglandin AL-6598 and quantitative autoradiographic visualization of DP and EP2 receptor sites in human eyes. Sharif, N.A., Williams, G.W., Crider, J.Y., Xu, S.X., Davis, T.L. Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics. (2004) [Pubmed]
Pharmacological characterization of [(3)H]-prostaglandin E(2) binding to the cloned human EP(4) prostanoid receptor. Davis, T.L., Sharif, N.A. Br. J. Pharmacol. (2000) [Pubmed]
Affinities, selectivities, potencies, and intrinsic activities of natural and synthetic prostanoids using endogenous receptors: focus on DP class prostanoids. Sharif, N.A., Crider, J.Y., Xu, S.X., Williams, G.W. J. Pharmacol. Exp. Ther. (2000) [Pubmed]

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