(±)-Talinolol

A β1-adrenergic receptor blocker

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库存: 现货

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1mg

￥437.00

350.00

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5mg

￥1850.00

1480.00

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10mg

￥3325.00

2660.00

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货号: ajci14416
CAS: 57460-41-0
别名: 他林洛尔,Cordanum
分子式: C20H33N3O3
分子量: 363.5
纯度: >98%
溶解度: ≤10mg/ml in ethanol;15mg/ml in DMSO;30mg/ml in dimethyl formamide
储存: Store at -20°C
库存: 现货

Background

(±)-Talinolol is a selective β1 adrenoceptor antagonist with cardioprotective and antihypertensive activity.

β adrenoceptor antagonist is a class of medications that are particularly used to manage cardiac arrhythmias, and to protect the heart from a second heart attack after a first heart attack.

By blocking β1-adrenergic receptors, (±)-talinolol delays the conduction of stimuli in the AV node, reduces the sino-atrial conduction time, and impedes the sinus node automaticity [1]. Pharmacokinetic data of the time course of plasma concentrations following intravenous infusion of 30 mg (±)-Talinolol revealed that the peak serum concentration (Cmax), the area under the serum concentration-time curve (AUC), and terminal elimination halflife (t1/2) were 631±95 ng/ml, 1433±153 ng×h/ml, and 10.6±3.3 h, respectively. Pharmacokinetic data of the time course of plasma concentrations following oral administration of 50 mg (±)-Talinolol revealed that the Cmax, the AUC, and the t1/2 were 168±67 ng/ml, 1321±382 ng×h/ml, and 11.9±2.4 h, respectively [2].

参考文献:
[1] Abmann I.? The actions of talinolol, a β1-selective beta blocker, in cardiac arrhythmia and acute myocardial infarction[J]. Current Medical Research and Opinion, 2008, 13(6): 325-342.
[2] Trausch B, Oertel R, Richter K, et al.? Disposition and bioavailability of the β1‐adrenoceptor antagonist talinolol in man[J]. Biopharmaceutics & Drug Disposition, 1995, 16(5): 403-414.