Uses
BW 245C is a DP agonist, affecting the signaling pathway on primary cultured rat hippocampal neuron injuries.
Definition
ChEBI: (3R,4S)-BW 245C is a 7-[3-(3-cyclohexyl-3-hydroxypropyl)-2,5-dioxoimidazolidin-4-yl]heptanoic acid that is the (3R,4S)-enantiomer of BW 245C. It is an enantiomer of a (3S,4R)-BW 245C.
Biological Activity
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].
References
[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.
