Alprenolol

Alprenolol is a non-selective β-adrenergic receptor (β-AR) antagonist that is also an antagonist of the serotonin (5-HT) receptor subtypes 5-HT_1A and 5-HT_1B.^1,2 It binds to β₁-, β₂-, and β₃-ARs expressed in CHO cells (K_ds = 15, 0.91, and 117 nM, respectively, for the human receptors) and to 5-HT_1A and 5-HT_1B receptors in rat hippocampal and striatal membranes (K_is = 34 and 134 nM, respectively).^1,2 In vivo, alprenolol (40 mg/kg, i.v.) completely blocks the hyperactivity response of rats to 2-PCPA (Item No. 10010494) and L-tryptophan.³ Alprenolol (10 μg, i.v.) inhibits decreases in heart rate and left ventricular systolic pressure induced by the β₂-AR antagonist ICI 118551 (Item No. 15591) in transgenic mice overexpressing the β₂-AR.⁴ It also reduces the level of abnormal prion fibrils (PrP^Sc) in the brain of mice intracerebrally infected with prion disease to less than 20% of control levels when administered in drinking water at a dose of 50 mg/L.⁵

WARNING This product is not for human or veterinary use.

1. Baker, J.G. The selectivity of β-adrenoceptor antagonists at the human β1, β₂ and β3 adrenoceptors. Br. J. Pharmacol. 144(3), 317-322 (2005).

2. Langlois, M., Brémont, B., Rousselle, D., et al. Structural analysis by the comparative molecular field analysis method of the affinity of β-adrenoreceptor blocking agents for 5-HT_1A and 5-HT_1B receptors. Eur. J. Pharmacol. 244(1), 77-87 (1993).

3. Costain, D.W., and Green, A.R. β-Adrenoceptor antagonists inhibit the behavioural responses of rats to increased brain 5-hydroxytryptamine. Br. J. Pharmacol. 64(2), 193-200 (1978).

4. Bond, R.A., Leff, P., Johnson, T.D., et al. Physiological effects of inverse agonists in transgenic mice with myocardial overexpression of the β₂-adrenoceptor. Nature 374(6519), 272-276 (1995).

5. Miyazaki, Y., Ishikawa, T., Kamatari, Y.O., et al. Identification of alprenolol hydrochloride as an anti-prion compound using surface plasmon resonance imaging. Mol. Neurobiol. (2018).