Background:

Target: DP1 receptor

IC50: 2.5 nM

Ki: 0.9 nM

BW 245C is a kind of prostaglandin analogue with stable chemical properties which functions as a potent inhibitor of platelet aggregation. BW 245C could selectively active the DP1 receptor, and inhibit [3H]-PGD2 binding to isolated human platelet membranes, with the Ki value of 0.9 nM [1].

In Vitro: BW 245C could inhibit the aggregation of human and rat platelets induced by ADP in a dose dependent manner, with the IC50 values of 8.7 nM and 9.9 nM, respectively [1]. Besides, in HEK293 cells stably expressing the hDP receptor, BW 245C could significantly increase cAMP production, with the EC50 value of 0.7 nM [2].

In Vivo: In spontaneously hypertensive rats, intravenous bolus injection with BW 245C at the dose of 250 μg/kg could reduce the systolic and diastolic blood pressure by 23% and 34%, respectively [1].

Clinical trial: In four healthy male volunteers, intravenous injection of BW 245C (1, 2 and 4 ng kg-1 min-1) exerted a progressive increase in heart rate and pulse pressure [3].

参考文献:
[1] Town H C, Casalsstenzel J, Schillinger E, et al.  Pharmacological and cardiovascular properties of a hydantoin derivative, BW 245 C, with high affinity and selectivity for PGD2 receptors[J]. Prostaglandins, 1983, 25(1): 13-28.
[2] Boie Y, Sawyer N, Slipetz D, et al.  MOLECULAR CLONING AND CHARACTERIZATION OF THE HUMAN PROSTANOID DP RECEPTOR[J]. Journal of Biological Chemistry, 1995, 270(32): 18910-18916.
[3] Orchard M A, Ritter J M, Shepherd G L, et al.  Cardiovascular and platelet effects in man of BW 245C, a stable mimic of epoprostenol (PGI2)[J]. British journal of clinical pharmacology, 1983, 15(5): 509-511.