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The synthesis of a novel thromboxane receptor antagonist 4(Z)-6-(2-o-chlorophenyl-4-o-hydroxyphenyl-1,3-dioxan-cis-5-yl) hexenoic acid ICI 192605.

Authors :
Brewster AG
Brown GR
Foubister AJ
Jessup R
Smithers MJ
Source :
Prostaglandins [Prostaglandins] 1988 Aug; Vol. 36 (2), pp. 173-8.
Publication Year :
1988

Abstract

The synthesis and summary pharmacology of a novel thromboxane receptor antagonist 4(Z)-6-(2-o-chlorophenyl-4-o-hydroxyphenyl-1, 3-dioxan-cis-5-yl) hexenoic acid (3) is reported. Compound 3 was competitive and selective with pA2 values of 8.0 +/- 0.1 (rabbit) and 8.4 +/- 0.05 (rat) on smooth muscle preparations and 8.16 +/- 0.01 on human platelets. In vivo activity of 3 was demonstrated in a Konzett Rossler guinea pig model at 0.01 mg/kg p.o.

Details

Language :
English
ISSN :
0090-6980
Volume :
36
Issue :
2
Database :
MEDLINE
Journal :
Prostaglandins
Publication Type :
Academic Journal
Accession number :
2973084
Full Text :
https://doi.org/10.1016/0090-6980(88)90304-8