4-Hydroxypropranolol (hydrochloride)

4-Hydroxypropranolol hydrochloride is a non-cardiac selective β-adrenergic receptor antagonist and a metabolite produced after oral administration of Propranolol (HY-B0573B). 4-Hydroxypropranolol hydrochloride also acts as a membrane stabilizer and possesses intrinsic sympathomimetic inhibitory activity. 4-Hydroxypropranolol hydrochloride blocks β-adrenergic receptors to antagonize the effects of catecholamines, acts as a partial β-adrenergic receptor agonist, and induces membrane stabilization. 4-Hydroxypropranolol hydrochloride alters heart rate, left ventricular contractility, and atrioventricular conduction time. 4-Hydroxypropranolol hydrochloride can be used in research related to cardiovascular and cerebrovascular diseases^[1][2]. IC50 & Target:pA2: 8.24 (β1-adrenergic receptor) and 8.26 (β2-adrenergic receptor)^[2] In Vivo:4-Hydroxypropranolol (54 μg/kg, i.v.) hydrochloride achieves 50% inhibition of Isoprenaline (HY-108353)-induced tachycardia in anesthetized cats^[1].
4-Hydroxypropranolol (10-80 μg/kg; i.v.) hydrochloride possesses intrinsic sympathomimetic activity, which causes a dose-dependent increase in heart rate in catecholamine-depleted rats^[1].
4-Hydroxypropranolol (0.025-0.8 mg/kg, s.c.) hydrochloride antagonizes the protective effect of isoprenaline against histamine-induced bronchospasm in guinea pigs^[1].
4-Hydroxypropranolol (0.09-13.25 mg/kg, i.v.) hydrochloride exerts β-adrenergic receptor blocking activity and membrane-stabilizing activity, thereby producing dose-dependent cardiovascular effects in normal anesthetized dogs, including decreased heart rate, reduced contractility, diminished aortic blood flow, and prolonged atrioventricular conduction time^[1].