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Partial Agonist Effects of BW A868C, a Selective DP Receptor Antagonist, on Cl- Secretion in Dog Tracheal Epithelium

Partial Agonist Effects of BW A868C, a Selective DP Receptor Antagonist, on Cl- Secretion in Dog Tracheal Epithelium

Y J Liu, D M Jackson, A Blackham, P Leff

Eur J Pharmacol. 1996 May 23;304(1-3):117-22.

PMID: 8813592

Abstract:

We examined the interactions of prostaglandin D2, BW245C ((+/-)-5-(6-carboxyhexyl)-1-(3-cyclohexyl-3-hydroxypropyl)-hydantoin) a selective DP receptor agonist and BW A868C ((+/-)-3-benzyl-5-(6-carboxyhexyl)-1-(2-cyclohexyl-2- hydroxyethylamino)-hydantoin) a selective DP receptor antagonist on Cl- secretion using dog isolated tracheal epithelial preparations in Ussing chambers. Both prostaglandin D2 and BW245C stimulated Cl- secretion as reflected by increased short-circuit current (Isc) in the epithelial cells where the latter was more potent than the former. BW A868C produced, consistently, weak but significant partial agonism on Cl- secretion in these preparations in addition to its expected antagonism at the DP receptors. A pKB estimate of 8.16 +/- 0.06 (n = 11) for BW A868C from its antagonism to BW245C was found to be comparable with its estimates of both p[A]50 (8.19 +/- 0.14, n = 5) and pKA (8.00 +/- 0.20, n = 5). In addition, no significant effect by BW A868C up to 1 microM on Cl- secretory responses to other prostanoids, such as prostaglandin E2, prostaglandin F2 alpha and 9 alpha, 11 beta-prostaglandin F2 alpha, was detected in the system. These results are consistent with previous findings that BW A868C is a selective antagonist at the DP receptors mediating Cl- secretion by epithelial cells. To our knowledge, this is a (the first) confirmation of partial agonist properties of BW A868C in an isolated tissue system.

Chemicals Related in the Paper:

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

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