Lofexidine (hydrochloride)
(Synonyms: 盐酸洛非西定; Baq-168; MDL-14042) 目录号 : GC17064
An α2-adrenergic receptor agonist
Cas No.:21498-08-8
Sample solution is provided at 25 µL, 10mM.
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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.
| 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 |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 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。 |
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| 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。 | ||
| 制备储备液 | |||
 |
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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet