Chlorcyclizine (hydrochloride)
(Synonyms: 盐酸氯环利嗪；盐酸氯环力嗪) 目录号 : GC13465
A histamine H1 antagonist
Cas No.:14362-31-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Rats[1]Timed-mated CRL:CD [SD] female rats between 9 and 13 weeks of age at initiation of dosing and weighing between 245 and 363 g are used. Rats are administered a single daily oral gavage dose of 30, 60, or 90 mg/kg Chlorcyclizine (n=8/group) during the sensitive period for palate development, GDs 11 to 14. These doses are selected such that 30 mg/kg is a likely no-effect dose and higher doses of 60 and/or 90 mg/kg will induce a moderate or high incidence of fetal cleft palate. Given that CRL:CDs [SD] rats have an extremely low incidence of spontaneous cleft palate in the testing laboratory, as well as to avoid unnecessary use of animals, a methylcellulose control group is omitted[1]. |
References: [1]. Enright BP, et al. Effects of the histamine H1 antagonist Chlorcyclizine on rat fetal palate development. Birth Defects Res B Dev Reprod Toxicol. 2010 Dec;89(6):474-84. | |
Chlorcyclizine is a phenylpiperazine antagonist for histamine H1 receptor [1].
The histamine has been involved in modulating many physiological functions of the hypothalamus, such as arousal state, feeding, locomotor activity, and drinking. Histamine has been involved in circadian rhythm of locomotor activity and exploratory behavior through H1R [1].
In vitro: The Ki value of chlorcyclizine for histamine H1 receptor was 9 nM [1]. Chlorcyclizin was effective against hepatitis C virus (HCV) with an EC50 of 44 nM, preventing viral entry into host cells [2].
In vivo: In chimeric mice xenografted with primary human hepatocytes, chlorcyclizine (10-50 mg/kg) significantly inhibited infection of HCV genotypes 1b and 2a [2]. Chlorcyclizine induced a resistance to sodium pentobarbital anesthesia. Intraperitoneal injection of chlorcyclizine showed a sedative effect in small doses, but a convulsive effect in large doses. Intraperitoneal injections of the drug did not affect the recovery time from pentobarbital anesthesia [3]. In rats, pretreatment with chlorcyclizine for several days shortened the duration of action of a subsequent dose of hexobarbital, pentobarbital or zoxazolamine, and accelerated in vivo metabolism of hexobarbital [4]. The administration of chlorcyclizine (50 g/kg) to rats by stomach tube daily for 1 week resulted in significant increases in liver weight, microsomal protein concentration and the activity of the NADPH-dependent hepatic microsomal ethanol-oxidizing system (MEOS) [5].
References:
[1] Tran V T, Chang R S, Snyder S H. Histamine H1 receptors identified in mammalian brain membranes with [3H] mepyramine[J]. Proceedings of the National Academy of Sciences, 1978, 75(12): 6290-6294.
[2] He, S. ,Xiao, J.,Dulcey, A.E., et al. Discovery, optimization, and characterization of novel chlorcyclizine derivatives for the treatment of hepatitis C virus infection. Journal of Medicinal Chemistry 59(3), 841-853 (2016).
[3] Thompson I D, Dolowy W C, Cole W H. Development of a resistance to sodium pentobarbital in rats fed on a diet containing chlorcyclizine hydrochloride[J]. Journal of Pharmacology and Experimental Therapeutics, 1959, 127(2): 164-166.
[4] Conney A H, Burns J J, Michaelson I A. Stimulatory effect of chlorcyclizine on barbiturate metabolism[J]. Journal of Pharmacology and Experimental Therapeutics, 1961, 132(2): 202-206.
[5] Khanna J M, Kalant H, Lin G. Significance in vivo of the increase in micro-somal ethanol-oxidizing system after chronic administration of ethanol, pheno-barbital and chlorcyclizine[J]. Biochemical pharmacology, 1972, 21(16): 2215-2226.
| Cas No. | 14362-31-3 | SDF | |
| 别名 | 盐酸氯环利嗪；盐酸氯环力嗪 | ||
| 化学名 | 1-[(4-chlorophenyl)phenylmethyl]-4-methyl-piperazine, monohydrochloride | ||
| Canonical SMILES | CN1CCN(C(C2=CC=C(Cl)C=C2)C3=CC=CC=C3)CC1.Cl | ||
| 分子式 | C18H21ClN2 • HCl | 分子量 | 337.3 |
| 溶解度 | ≥ 11mg/mL in DMSO with gentle warming | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9647 mL | 14.8236 mL | 29.6472 mL |
| 5 mM | 0.5929 mL | 2.9647 mL | 5.9294 mL |
| 10 mM | 0.2965 mL | 1.4824 mL | 2.9647 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。
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