Pindolol

Pindolol is an antagonist of β₁- and β₂-adrenergic receptors (β₁- and β₂-ARs; K_is = 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-HT_1A receptor (K_i = 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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1. Hicks, P.E., Cavero, I., Manoury, P., et al. Comparative analysis of beta-1 adrenoceptor agonist and antagonist potency and selectivity of cicloprolol, xamoterol and pindolol. J. Pharmacol. Exp. Ther. 242(3), 1025-1034 (1987).

2. Hoffmann, C., Leitz, M.R., Oberdorf-Maass, S., et al. Comparative pharmacology of human β-adrenergic receptor subtypes—characterization of stably transfected receptors in CHO cells. N.-S. Arch. Pharmacol. 369(2), 151-159 (2004).

3. Krushinski, J.H., Jr., Schaus, J.M., Thompson, D.C., et al. Indoloxypropanolamine analogues as 5-HT_1A receptor antagonists. Bioorg. Med. Chem. Lett. 17(20), 5600-5604 (2007).

4. Lubawski, I., and Wale, J. Studies with LB 46, a new β-receptor blocking drug. Eur. J. Pharmacol. 6(3), 345-348 (1969).

5. Antonaccio, M.J., High, J., DeForrest, J.M., et al. Antihypertensive effects of 12 beta adrenoceptor antagonists in conscious spontaneously hypertensive rats: Relationship to changes in plasma renin activity, heart rate and sympathetic nerve function. J. Pharmacol. Exp. Ther. 238(1), 378-387 (1986).