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Pindolol is an antagonist of β1- and β2-adrenergic receptors (β1- and β2-ARs; Kis = 2.6 and 4.8 nM, respectively) and a partial agonist of the β3-AR, stimulating adenylyl cyclase in membranes of cells expressing the human receptor.[1],[2] It is also an antagonist of the serotonin 5-HT1A receptor (Ki = 81.1 nM for inhibition of 5-HT-stimulated GTPγS binding).[3] Pindolol inhibits isoproterenol-induced tachycardia in anesthetized cats (ED50 = 1.8 µg/kg).[4] It also decreases mean blood pressure in conscious spontaneously hypertensive rats when administered at a dose of 30 mg/kg per day, but concomitantly increases heart rate.[5] Formulations containing pindolol have been used in the treatment of hypertension.

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