产品描述:
BIBS39 is a nonpeptide antagonist of the angiotensin II type 1 (AT1) receptor (Ki = 29 nM in rat lung membranes).{46447} It is selective for AT1 over AT2 receptors (Ki = 480 nM in isolated rat adrenal medulla), as well as α1-, α2-, β1-, and β2-adrenergic, adenosine A1 and A2, muscarinic M1, M2, and M3, and atrial natriuretic peptide receptors (Kis = >100 µM for all). BIBS39 (0.3-10 mg/kg) decreases diastolic blood pressure in pithed normotensive rats without affecting heart rate and in renal hypertensive rats with an increase in heart rate when administered at doses ranging from 1 to 30 mg/kg.{46447,46448}