Novel human metabolites of the angiotensin-II antagonist tasosartan and their pharmacological effects
Bioorganic & Medicinal Chemistry Letters(2002)
Abstract
Three novel metabolites of the angiotensin-II (A-II) receptor antagonist tasosartan have been identified in humans, and the syntheses and pharmacologic profiling of these metabolites are reported. Each metabolite bound the human A-II receptor with IC50s between 20 and 45nM. The in vivo effects of these compounds in attenuating the pressor response to angiotensin-II challenge in anesthetized rats were also investigated. An unsaturated diol metabolite exhibited in vivo efficacy at intravenous doses of 1 and 3mg/kg, while the other metabolites, both carboxylic acids, had no significant effect at the same doses.
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Key words
angiotensin-ii angiotensin-ii,novel human metabolites,pharmacological effects
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