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The Classification of Prostaglandin DP-receptors in Platelets and Vasculature Using BW A868C, a Novel, Selective and Potent Competitive Antagonist

The Classification of Prostaglandin DP-receptors in Platelets and Vasculature Using BW A868C, a Novel, Selective and Potent Competitive Antagonist

H Giles, P Leff, M L Bolofo, M G Kelly, A D Robertson

Br J Pharmacol. 1989 Feb;96(2):291-300.

PMID: 2924081

Abstract:

1. BW A868C, a novel compound, behaved as a simple competitive antagonist in a human washed platelet aggregation assay. Anti-aggregatory concentration-effect curves to BW 245C were displaced in a parallel manner. The shifts accorded with a Schild plot slope of unity and a pKB of 9.26. 2. Inhibition of platelet aggregation by prostaglandin D2 (PGD2) was antagonized with a similar potency, as were the relaxation effects of BW 245C and PGD2 in the rabbit jugular vein. BW A868C can, therefore, be classified as a DP-receptor antagonist. 3. Actions of BW A868C at other prostaglandin receptors (IP, EP1, EP2, TP and FP) were excluded at concentrations up to 1,000 times higher than the DP-receptor affinity. 4. Analyses of BW 245C- and PGD2-mediated effects were complicated by additional agonist receptor interactions which were revealed by BW A868C. In rabbit jugular vein a resistant phase of agonism was detectable, indicating that both agonists exerted effects through another receptor (possibly EP2). Also, PGD2, in addition to its anti-aggregatory effect on platelets, demonstrated a pro-aggregatory action in the presence of BW A868C. 5. The contractile effects of PGD2 in guinea-pig tracheal strips were resistant to 10 microM BW A868C indicating that they were not mediated through DP-receptors. 6. To our knowledge this is the first account of a well-classified competitive antagonist at the DP-receptor. Its potency and selectivity make it an important new tool in prostanoid receptor classification and identification.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP118675506	BW A868C		118675-50-6	Price

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