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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.
- 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.
- Subjects :
- 15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid
Animals
Humans
Prostaglandin Endoperoxides, Synthetic pharmacology
Rabbits
Receptors, Prostaglandin drug effects
Receptors, Thromboxane
Dioxanes chemical synthesis
Dioxins chemical synthesis
Receptors, Prostaglandin metabolism
Subjects
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