tcsc2680 Propranolol (hydrochloride)

Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist with an IC₅₀ of 12 nM.

IC50 & Target: IC50: 12 nM (βAR)^[1]

In Vitro: In cultured endothelial or tumor cells, propranolol has been shown to both reduce cAMP levels and simultaneously activate the mitogen-activated protein kinase (MAPK) pathway downstream of βAR inhibition^[2]. It displays high affinity for 5-HT_1B receptors (K_i= 17 nM), and milder affinity for 5HT_1D receptors (K_i= 10.2 μM)^[3].

In Vivo: Chronic administration of propranolol increased the beta(1)-adrenoceptors but decreased the beta(2)-adrenoceptors without changing total amount of plasma membrane beta-adrenoceptors^[4].