Distinct effects of Z-335, a new thromboxane A2 receptor antagonist, on rabbit platelets and aortic smooth muscle

Makoto Yoshida, Yukari Sato, Tokuro Shimura, Satoko Ohkubo, Shigeyoshi Honma, Takao Tanaka, Tadashi Kurimoto, Norimichi Nakahata

Research output: Contribution to journalArticlepeer-review

4 Citations (Scopus)

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 languageEnglish
Pages (from-to)50-56
Number of pages7
JournalPharmacology
Volume79
Issue number1
DOIs
Publication statusPublished - 2007 Jan

Keywords

  • Aggregation
  • Aortic smooth muscle cells
  • Constriction
  • Platelets
  • Thromboxane A

ASJC Scopus subject areas

  • Pharmacology

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