Labetalol (AH5158) is an orally active selective α1- and non-selective β-adrenergic receptors competitive antagonist. Labetalol, an anti-hypertensive agent, can be used for the research of cardiovascular disease, such as hypertension in pregnancy.
性状
Solid
IC50 & Target[1][2]
α1-adrenergic receptor β-adrenoceptor
体外研究(In Vitro)
Labetalol exhibits greater affinity for β-adrenergic sites on guinea pig heart and lung membranes (IC50=0.8 and 4.0 μM respectively) .Labetalol has affinity for α-adrenergic binding sites (IC50=15 uM) on rabbit uterine membranes.Labctalol has 19 times greater binding affinity for β binding sites in heart membranca than α binding sites in uterine membranes. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Labetalol (10 mg/kg; i.h.) passes the blood-brain barrier, reaching a level of 2.1 ug/g tissue in the 10-day-old rat pups brain 90 min after injection.
Labetalol (5.0 mg/kg; i.p.) attenuates circulating IL-1β and IL-6 in tailshock stress rats. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Brogden RN, et al. Labetalol: a review of its pharmacology and therapeutic use in hypertension. Drugs. 1978;15(4):251-270.[2]. Greenslade FC, et al. Labetalol binding to specific alpha- and beta-adrenergic sites in vitro and its antagonism of adrenergic responses in vivo. J Mol Cell Cardiol. 1979 Aug;11(8):803-11.
溶解度数据
In Vitro: DMSO : 125 mg/mL (380.62 mM; Need ultrasonic)配制储备液