Novel human metabolites of the angiotensin-II antagonist tasosartan and their pharmacological effects.

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Elokdah HM, Friedrichs GS, Chai SY, Harrison BL, Primeau J, Chlenov M, Crandall DL

Novel human metabolites of the angiotensin-II antagonist tasosartan and their pharmacological effects.

Bioorg Med Chem Lett. 2002 Aug 5;12(15):1967-71.

PubMed ID

12113820 [View in PubMed

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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 IC(50)s 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.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Tasosartan	Type-1 angiotensin II receptor	Protein	Humans	Yes	Antagonist	Details

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Tasosartan	Type-1 angiotensin II receptor	IC 50 (nM)	38	N/A	N/A	Details