Pharmacology and autoradiography of human DP prostanoid receptors using [3 H]-BWA868C, a DP receptor-selective antagonist radioligand
نویسندگان
چکیده
منابع مشابه
The role of the prostaglandin D2 receptor, DP, in eosinophil trafficking.
Prostaglandin (PG) D2 is a major mast cell product that acts via two receptors, the D-type prostanoid (DP) and the chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2) receptors. Whereas CRTH2 mediates the chemotaxis of eosinophils, basophils, and Th2 lymphocytes, the role of DP has remained unclear. We report in this study that, in addition to CRTH2, the DP receptor play...
متن کاملAffinities, selectivities, potencies, and intrinsic activities of natural and synthetic prostanoids using endogenous receptors: focus on DP class prostanoids.
The prostanoid receptor-subtype binding affinities, selectivities, potencies, and intrinsic activities of four natural prostanoids and six synthetic DP class prostanoids were determined using binding and functional assays with endogenous receptors. SQ27986 exhibited the highest affinity for the human platelet DP receptor and the best DP receptor selectivity profile. Prostaglandin (PG)D(2) was t...
متن کاملEffects of PGH2 and PGD2 on CRTH2 and DP receptors in primary cells and co-expressed in HEK293 cells
Prostaglandin (PG) D2 is a PGH2 metabolite deriving from the cyclooxygenase pathway and the major prostanoid released from activated human mast cells. The biological effects of PGD2 are mediated by the G protein-coupled receptors (GPCRs) D-type prostanoid receptor (DP) and the chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2). Eosinophils, important effector cells in a...
متن کاملPredicting the Drug Interaction Potential of AMG 853, a Dual Antagonist of the D-Prostanoid (DP) and Chemoattractant Receptor-Homologous Molecule Expressed on TH2 Cells (CRTH2) Receptors
curve; C max , peak drug concentration observed in plasma This article has not been copyedited and formatted. The final version may differ from this version. Abstract AMG 853 is an orally bioavailable and potent dual antagonist of the D-prostanoid (DP) and chemoattractant receptor-homologous molecule expressed on TH2 cells (CRTH2) receptors. The drug interaction potential of AMG 853, both as a ...
متن کاملProstanoid-induced relaxation of precontracted cat ciliary muscle is mediated by EP2 and DP receptors.
The pharmacology of prostanoid-induced relaxation of the precontracted cat ciliary smooth muscle was characterized using synthetic prostaglandin (PG) analogues that are selective for specific prostanoid receptors. Relaxation was studied using carbachol to precontract the isolated longitudinal ciliary muscle, followed by application of the PG agonist. Of the compounds studied, PGE2 was the most ...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: British Journal of Pharmacology
سال: 2000
ISSN: 0007-1188
DOI: 10.1038/sj.bjp.0703686