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Effects of BW A868C, a selective prostaglandin DP receptor antagonist, in dog isolated vascular preparations
- Source :
- European Journal of Pharmacology. 303:187-192
- Publication Year :
- 1996
- Publisher :
- Elsevier BV, 1996.
-
Abstract
- The effects of the selective prostaglandin DP receptor antagonist BW A868C ((+/-)-3-benzyl-5-(6-carboxyhexyl)-1-(2-cyclohexyl-2-hydroxyethylamin o)- hydantoin), 3.0 nM to 0.3 microM) were examined against prostaglandin D2 and BW245C ((+/-)-5-(6-carboxyhexyl)-1-(3-cyclohexyl-3-hydroxypropyl)-hydantoin)-in duced smooth muscle relaxation on dog isolated vascular preparations pre-contracted with a sub-maximal concentration of KCl (50 mM). In dog dorsal nasal vein BW245C was found to be more potent than prostaglandin D2 with p[A]50 estimates of 7.6 +/- 0.1 (S.E.M., n = 8) and 5.8 +/- 0.1 (n = 5), respectively. BW A868C, up to 0.3 microM, displaced the relaxant concentration-effect curves to BW245C in dog dorsal nasal vein in an apparently competitive manner with parallel rightward shifts and no significant changes in the upper asymptotes. The data were analysed by using a modified Schild equation which not only gives equal weight to all agonist concentration-effect data but also allows a direct plot in Clark plot space. A pKB estimate of 7.3 +/- 0.8 (n = 20) was obtained with a unity Schild plot slope (b = 1.0 +/- 0.1). This affinity estimate, however, is lower than the values previously reported in other studies. The affinity estimates of BW A868C against BW245C and prostaglandin D2 obtained from dog dorsal nasal vein, major palatine artery and saphenous vein were found to be consistent. The relatively low affinity estimates of BW A868C at DP receptors as observed in the present study may be due to species- or tissue-related variations or may be indicative of the possible existence of DP receptor subtypes.
- Subjects :
- Male
Pharmacology
Agonist
medicine.medical_specialty
biology
Chemistry
medicine.drug_class
Hydantoins
Fissipedia
Antagonist
In Vitro Techniques
biology.organism_classification
Schild regression
chemistry.chemical_compound
Dogs
Endocrinology
Mechanism of action
Internal medicine
medicine
Carnivora
Animals
Female
Prostaglandin D2
medicine.symptom
Receptor
Subjects
Details
- ISSN :
- 00142999
- Volume :
- 303
- Database :
- OpenAIRE
- Journal :
- European Journal of Pharmacology
- Accession number :
- edsair.doi.dedup.....479afb9fd81300c6eccfce1620c23672