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Lofexidine(hydrochloride)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Lofexidine(hydrochloride)图片
CAS NO:21498-08-8
包装与价格:
包装价格(元)
10mM (in 1mL Water)电议
50mg电议

产品介绍
洛非西定(盐酸盐)是一种选择性 α2 受体激动剂,通常用于缓解海洛因和其他类型阿片类药物戒断的身体症状。
Cas No.21498-08-8
别名盐酸洛非西定; Baq-168; MDL-14042
化学名2-[1-(2,6-dichlorophenoxy)ethyl]-4,5-dihydro-1H-imidazole, monohydrochloride
Canonical SMILESClC1=CC=CC(Cl)=C1OC(C)C2=NCCN2.Cl
分子式C11H12Cl2N2O o HCl
分子量295.6
溶解度≥ 11.15mg/mL in Water
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Lofexidine is a α2-Receptor agonist for opioid detoxification. Lofexidine shows a strong affinity for the α2A-receptor subtype [1].

The α2 adrenergic receptor is a G protein-coupled receptor (GPCR) consisting three highly homologous subtypes, α2A-, α2B-, and α2C-adrenergic. The α-receptors in brain are important presynaptic modulators of central noradrenergic function (autoreceptors) and postsynaptic mediators of many effects of catecholamines and related drugs. The α2-adrenergic agonists can be used as antihypertensives and preanesthetic agents [2].

Lofexidine is extensively absorbed, reaching peak concentrations at approximately 3 hours after oral administration. The mean maximum serum concentrations following a single 1.2 or 2.0 mg dose in healthy male adults were 1755 ± 306 and 2795 ± 593 ng/ml, respectively [1].

Clinical trials: Lofexidine has entered clinical trials in the patients treatment of opiate withdrawal. Lofexidine-treated patients experienced a rebound increase in blood pressure following discontinuation of lofexidine. The most frequently reported adverse events were insomnia, dry mucous membranes, sedation, dizziness, and asthenia [1].

References:
[1] Gish E C, Miller J L, Honey B L, et al.  Lofexidine, an α2-receptor agonist for opioid detoxification[J]. Annals of Pharmacotherapy, 2010, 44(2): 343-351.
[2] Scheinin M, Lomasney J W, Hayden-Hixson D M, et al.  Distribution of α2-adrenergic receptor subtype gene expression in rat brain[J]. Molecular Brain Research, 1994, 21(1): 133-149.