Literature DB >> 2973084

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.

A G Brewster1, G R Brown, A J Foubister, R Jessup, M J Smithers.   

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.

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Year:  1988        PMID: 2973084     DOI: 10.1016/0090-6980(88)90304-8

Source DB:  PubMed          Journal:  Prostaglandins        ISSN: 0090-6980


  4 in total

1.  Vasoconstrictor responses, and underlying mechanisms, to isoprostanes in human and porcine bronchial arterial smooth muscle.

Authors:  Tracy Tazzeo; John Miller; Luke J Janssen
Journal:  Br J Pharmacol       Date:  2003-09-22       Impact factor: 8.739

Review 2.  Prostanoid receptor antagonists: development strategies and therapeutic applications.

Authors:  R L Jones; M A Giembycz; D F Woodward
Journal:  Br J Pharmacol       Date:  2009-07-15       Impact factor: 8.739

3.  Effects of a thromboxane receptor antagonist on prostaglandin D2 and histamine induced bronchoconstriction in man.

Authors:  N al Jarad; K P Hui; N Barnes
Journal:  Br J Clin Pharmacol       Date:  1994-01       Impact factor: 4.335

4.  Thromboxane A2 inhibition of SKCa after NO synthase block in rat middle cerebral artery.

Authors:  A J McNeish; C J Garland
Journal:  Br J Pharmacol       Date:  2007-04-10       Impact factor: 8.739

  4 in total

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