Biological Activity
bw a868c is a novel, selective and potent competitive antagonist of prostaglandin d2 (pgd2) [1].prostaglandin d2 has been widely distributed in rat brain, spinal cord and pituitary and may act as a neuromodulator in the central nervous system [2]. prostaglandin d2 is critical for the development of allergic diseases such as asthma.
in vitro
in glycerol-lysed human platelets, bw245c activated adenylate cyclase in a biphasic manner. bw a868c showed no effect on carbacyclin, iloprost, prostacyclin, pge1 and pge2 at a concentration 1,000 fold that of its kb against pgd2 and bw245c [1]. bw a868c showed no effect on human tp, ip, ep1, ep2, and fp receptors. the ki value for bw a868c is approximately 1.7 nm[1] .in isolated rings of rabbit saphenous vein (rbsv) pre-contracted with 40 mm kcl, bw245c caused concentration-dependent relaxations with an ec50 of 38 nm [3].
References
[1] giles h, leff p, bolofo m l, et al. the classification of prostaglandin dp‐receptors in platelets and vasculature using bw a868c, a novel, selective and potent competitive antagonist[j]. british journal of pharmacology, 1989, 96(2): 291-300.
[2] shimizu t, mizuno n, amano t, et al. prostaglandin d2, a neuromodulator[j]. proceedings of the national academy of sciences, 1979, 76(12): 6231-6234.
[3] lydford s j, mckechnie k c w, leff p. interaction of bw a868c, a prostanoid dp-receptor antagonist, with two receptor subtypes in the rabbit isolated saphenous vein[j]. prostaglandins, 1996, 52(2): 125-139.
