Cyclizine
(Synonyms: 苯甲嗪) 目录号 : GC64088
A histamine H1 receptor antagonist
Cas No.:82-92-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cyclizine is a histamine H1 receptor antagonist.1,2,3 It binds selectively to histamine H1 receptors (Kd = 5 nM) over H2 and H3 receptors (Kds = 1,600 and >580 nM, respectively).3 Cyclizine inhibits anti-IgE-induced histamine release from isolated human lung fragments with an IC50 value of 5.42 ?M but induces histamine release with a 50% release concentration (RC50) of 10.81 ?M.4 It reduces LPS-induced nitrite accumulation and protein levels of induced nitric oxide synthase (iNOS) in RAW 264.7 cells when used at a concentration of 100 nM.2 Cyclizine (10 and 20 mg/kg) reduces immobility in the forced swim test in rats.5
1.Hamlin, K.E., Weston, A.W., Fischer, F.E., et al.Histamine antagonists. II.1 Unsymmetrical 1,4-disubstituted piperazinesJ. Am. Chem. Soc.71(8)2731-2734(2019) 2.Králová, J., Ra?ková, L., Pekarová, M., et al.The effects of H1-antihistamines on the nitric oxide production by RAW 264.7 cells with respect to their lipophilicityInt. Immunopharmacol.9(7-8)990-995(2009) 3.Hill, S.J.Distribution, properties, and functional characteristics of three classes of histamine receptorPharmacol. Rev.42(1)45-83(1990) 4.Church, M.K., and Gradidge, C.F.Inhibition of histamine release from human lung in vitro by antihistamines and related drugsBr. J. Pharmacol.69(4)663-667(2019) 5.Khanwelkar, C.C., Gokhale, D.V., Santakke, A.V., et al.Effects of H1–receptor antagonists in antidepressant tests in ratsAl Ameen J. Med. Sci.1(2)84-92(2008)
| Cas No. | 82-92-8 | SDF | Download SDF |
| 别名 | 苯甲嗪 | ||
| 分子式 | C18H22N2 | 分子量 | 266.38 |
| 溶解度 | DMSO : 100 mg/mL (375.40 mM; Need ultrasonic) | 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 | 3.754 mL | 18.7702 mL | 37.5404 mL |
| 5 mM | 0.7508 mL | 3.754 mL | 7.5081 mL |
| 10 mM | 0.3754 mL | 1.877 mL | 3.754 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。
[Cyclizine is sold in Denmark as an over-the-counter drug and has serious side effects when overdosed]
Ugeskr Laeger 2018 Jan 15;180(3):V07170519.PMID:29336302doi
Cyclizine is sold in Denmark as an over-the-counter drug and affects not only histaminergic but also muscarinergic, serotonergic and α-adrenergic receptors, with side effects such as respiratory depression and cardiac arrhythmias, leading to fatalities. Due to the numerous side effects, it raises questions concerning the status of Cyclizine as an over-the-counter drug. Data of healthcare contacts because of Cyclizine intoxication in the 2014-2016 period should be analyzed to further illuminate the health risk of Cyclizine poisoning.
Cyclizine pharmacovigilance in hospice/palliative care: net effects for nausea or vomiting
BMJ Support Palliat Care 2022 Nov 10;bmjspcare-2022-003795.PMID:36357164DOI:10.1136/spcare-2022-003795.
Objectives: To describe the contemporary real-world use of Cyclizine for nausea or vomiting, and the associated benefits and harms. Methods: This was a prospective, consecutive case series of routine clinical use of Cyclizine for nausea or vomiting in palliative care conducted across 19 sites in Australia, Aotearoa/New Zealand and the UK. Clinical outcomes were graded using the National Cancer Institute Common Terminology Criteria for Adverse Events at baseline and 72 hours after initiation of Cyclizine. Ad hoc safety reporting continued for 2 weeks. Results: Data were collected from 101 patients between May 2018 and December 2020. Cyclizine was mostly used in combination with another antiemetic. Overall, 79 patients benefited and 32 experienced harm (56 had benefit without harm; 9 had harm without benefit). The most common harms were constipation (13%), somnolence (9%) and confusion (7%), adding to the already high rates of these symptoms at baseline. For the four patients with serious harms (grade ≥3), these were exacerbations of existing symptoms. Nine patients stopped Cyclizine at 72 hours and a further 20 patients within 2 weeks. The most common reasons for stopping were lack of benefit and symptom resolution; none stopped because of harms. Conclusions: When used as described in a palliative care setting, Cyclizine benefits about three-quarters of patients, with about one-third experiencing tolerable harms.
Post-operative Cyclizine misuse
Scott Med J 2013 Nov;58(4):e1-2.PMID:24215049DOI:10.1177/0036933013508039.
Cyclizine is commonly prescribed as an anti-emetic post-operatively. We report a case of a 51-year-old woman who developed addiction to intravenous Cyclizine following regular administration at recommended doses. This is the first report of Cyclizine misuse post-operatively. We compare this case to Cyclizine abuse reported amongst other populations. Prescribers should be aware of the potential of Cyclizine as a drug of abuse.
The cautious use of Cyclizine in a patient with myasthenia gravis
J Palliat Med 2009 Oct;12(10):879-80.PMID:19807233DOI:10.1089/jpm.2009.0028.
This brief report describes the cautious but successful use of Cyclizine, an anticholinergic agent, for the relief of intractable nausea in a patient with myasthenia gravis, followed by a review of the available literature.
Cyclizine abuse among a group of opiate dependents receiving methadone
Br J Addict 1989 Aug;84(8):929-34.PMID:2775912DOI:10.1111/j.1360-0443.1989.tb00766.x.
Twenty opiate dependents receiving long-term prescriptions of oral methadone, were identified as being habitual abusers of the anti-emetic drug Cyclizine. A semi-structured interview elicited the dosage of Cyclizine used, its effects, the reasons for starting and persisting with abuse of Cyclizine and the attitudes of the patients to it. Cyclizine was taken in large doses intravenously with methadone. The effects initially were of intense stimulation, often with hallucinations, sometimes with aggressive behaviour, and occasionally with epileptic fits. Subsequent depressive mood changes occurred often accompanied by a craving for Cyclizine. Tolerance to the drug occurred but no clear cut withdrawal syndrome is apparent. It seems that dependence upon Cyclizine occurs. The significance of these findings for doctors, pharmacists and for drug treatment units is discussed. The paucity of information on the pharmacology and pharmacokinetics is noted.