Tasosartan is an angiotensin II type 2 (AT2) receptor antagonist (IC50 = 1.2 nM in rat adrenal gland membranes).1 It also binds to the AT1 receptor (Ki = 46.6 nM in rat liver epithelial cells).2 Tasosartan (3 mg/kg, intraduodenally) reduces the AT2-induced pressor response in rats.3 It also decreases mean arterial pressure in a rat model of hypertension induced by renal artery constriction when administered intragastrically or intravenously at doses of 1 and 3 mg/kg.1
1.Ellingboe, J.W., Collini, M.D., Quagliato, D., et al.Metabolites of the angiotensin II antagonist tasosartan: The importance of a second acidic groupJ. Med. Chem.41(22)4251-4260(1998) 2.Hines, J., Fluharty, S.J., and Sakai, R.R.The angiotensin AT1 receptor antagonist irbesartan has near-peptide affinity and potently blocks receptor signalingEur. J. Pharmacol.384(1)81-89(1999) 3.Ellingboe, J.W., Antane, M., Nguyen, T.T., et al.Pyrido[2,3-d]pyrimidine angiotensin II antagonistsJ. Med. Chem.37(4)542-550(1994)