Abstract
The effect of a novel thromboxane A2 receptor (TP) antagonist, (±)-sodium[2-(4-chlorophenylsulfonylaminomethyl)- indan-5-yl]acetate monohydrate (Z-335), on the U46619-induced responses was compared between rabbit platelets and aorta. Z-335 inhibited platelet shape change induced by U46619 with higher efficacy than SQ29548, a common TP antagonist. The U46619-induced platelet aggregation was inhibited by Z-335 in a noncompetitive manner, while it was competitively inhibited by SQ29548. Z-335 inhibited U46619-induced vasoconstriction of rabbit aorta with higher efficacy than SQ29548. The pA 2 value of Z-335 in aortic vasoconstriction was significantly higher than in platelet shape change. The competitive binding study showed the higher pKi value of Z-335 against [3H]-SQ29548 binding in rabbit aortic smooth muscle cells than in platelets. These data suggest that Z-335 has useful characteristics of TP antagonism.
Original language | English |
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Pages (from-to) | 50-56 |
Number of pages | 7 |
Journal | Pharmacology |
Volume | 79 |
Issue number | 1 |
DOIs | |
Publication status | Published - 2007 Jan |
Keywords
- Aggregation
- Aortic smooth muscle cells
- Constriction
- Platelets
- Thromboxane A
ASJC Scopus subject areas
- Pharmacology