BW 245C is a selective agonist for the DP1 receptor.1,2 The Ki of BW 245C for the inhibition of [3H]-PGD2 binding to isolated human platelet membranes is 0.9 nM.1 It has a reported IC50 of 2.5 nM for the inhibition of ADP-induced human platelet aggregation3 and an IC50 of 250 nM for the inhibition of rat platelet aggregation.2
1
Boie, Y., Sawyer, N., Slipetz, D.M., et al. Molecular cloning and characterization of the human prostanoid DP receptor. J Biol Chem27018910-18916(1995).
2
Town, M., Casals-Stenzel, J., and Schillinger, E. Pharmacological and cardiovascular properties of a hydantoin derivative, BW 245 C, with high affinity and selectivity for PGD2 receptors. Prostaglandins2513-28(1983).
3
Narumiya, S., and Toda, N. Different responsiveness of prostaglandin D2-sensitive systems to prostaglandin D2 and its analogues. Br J Pharmacol85367-375(1985).
Narumiya, S., and Toda, N. Different responsiveness of prostaglandin D2-sensitive systems to prostaglandin D2 and its analogues. Br J Pharmacol85367-375(1985).
Boie, Y., Sawyer, N., Slipetz, D.M., et al. Molecular cloning and characterization of the human prostanoid DP receptor. J Biol Chem27018910-18916(1995).
Caldwell, A.G., Harris, C.J., Stepney, R., et al. Hydantoin prostaglandin analogues, potent and selective inhibitors of platelet aggregation. J Chem Soc Chem Commun561-562(1979).
Town, M., Casals-Stenzel, J., and Schillinger, E. Pharmacological and cardiovascular properties of a hydantoin derivative, BW 245 C, with high affinity and selectivity for PGD2 receptors. Prostaglandins2513-28(1983).
Tokumoto, H., Watanabe, Y., Yamashita, A., et al. Specificity of prostaglandin D2 binding to synaptic membrane fraction of rat brain. Brain Res362114-121(1986).