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

Article Details

Citation

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
]
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
DrugTargetKindOrganismPharmacological ActionActions
TasosartanType-1 angiotensin II receptorProteinHumans
Yes
Antagonist
Details
Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
TasosartanType-1 angiotensin II receptorIC 50 (nM)38N/AN/ADetails