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Lofexidine (hydrochloride) Sale

(Synonyms: 盐酸洛非西定; Baq-168; MDL-14042) 目录号 : GC17064

An α2-adrenergic receptor agonist

Lofexidine (hydrochloride) Chemical Structure

Cas No.:21498-08-8

规格 价格 库存 购买数量
10mM (in 1mL Water)
¥990.00
现货
50mg
¥900.00
现货

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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.

Chemical Properties

Cas No. 21498-08-8 SDF
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 SMILES ClC1=CC=CC(Cl)=C1OC(C)C2=NCCN2.Cl
分子式 C11H12Cl2N2O • HCl 分子量 295.6
溶解度 ≥ 11.15mg/mL in Water 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

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1 mg 5 mg 10 mg
1 mM 3.3829 mL 16.9147 mL 33.8295 mL
5 mM 0.6766 mL 3.3829 mL 6.7659 mL
10 mM 0.3383 mL 1.6915 mL 3.3829 mL
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