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药品详细

Cinnarizine(桂利嗪)

化学结构式图
中文名
桂利嗪
英文名
Cinnarizine
分子式
C26H28N2
化学名
1-(diphenylmethyl)-4-(3-phenylprop-2-en-1-yl)piperazine
分子量
Average: 368.5139
Monoisotopic: 368.225248906
CAS号
298-57-7
ATC分类
N07C 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Cinnarizine is an anti-histaminic drug which is mainly used for the control of vomiting due to motion sickness. Cinnarizine was first synthesized by Janssen Pharmaceutica in 1955.

It acts by interfering with the signal transmission between vestibular apparatus of the inner ear and the vomiting centre of the hypothalamus. The disparity of signal processing between inner ear motion receptors and the visual senses is abolished, so that the confusion of brain whether the individual is moving or standing is reduced. Vomiting in motion sickness is actually a physiological compensatory mechanism of the brain to keep the individual from moving so that it can adjust to the signal perception.

Cinnarizine could be also viewed as a nootropic drug because of its vasorelaxating abilities (due to calcium channel blockage), which happen mostly in brain. It is also effectively combined with other nootropics, primarily piracetam; in such combination each drug potentiate the other in boosting brain oxygen supply.

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference Not Available
    剂型
    规格
    化合物类型
    Type small molecule
    Classes
    • Diphenylmethanes
    Substructures
    • Alkanes and Alkenes
    • Phenylpropenes
    • Piperazines
    • Benzene and Derivatives
    • Aliphatic and Aryl Amines
    • Diphenylmethanes
    • Heterocyclic compounds
    • Aromatic compounds
    • Styrene Derivatives
    适应症
    药理
    Indication For the treatment of vertigo/meniere's disease, nausea and vomiting, motion sickness and also useful for vestibular symptoms of other origins.
    Pharmacodynamics Cinnarizine is an antihistamine and a calcium channel blocker. Histamines mediate a number of activities such as contraction of smooth muscle of the airways and gastrointestinal tract, vasodilatation, cardiac stimulation, secretion of gastric acid, promotion of interleukin release and chemotaxis of eosinophils and mast cells. Competitive antagonists at histamine H1 receptors may be divided into first (sedating) and second (non-sedating) generation agents. Some, such as Cinnarizine also block muscarinic acetylcholine receptors and are used as anti-emetic agents. Cinnarizine through its calcium channel blocking ability also inhibits stimulation of the vestibular system.
    Mechanism of action Cinnarizine inhibits contractions of vascular smooth muscle cells by blocking L-type and T-type voltage gated calcium channels. Cinnarizine has also been implicated in binding to dopamine D2 receptors, histamine H1 receptors, and muscarinic acetylcholine receptors.
    Absorption Not Available
    Volume of distribution Not Available
    Protein binding Not Available
    Metabolism
    Not Available
    Route of elimination Not Available
    Half life Not Available
    Clearance Not Available
    Toxicity Not Available
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    water solubility 750 mg/L (at 25 °C) YALKOWSKY,SH & DANNENFELSER,RM (1992)
    logP 5.77 BIOBYTE (1995)
    Predicted Properties
    Property Value Source
    water solubility 1.72e-03 g/l ALOGPS
    logP 5.19 ALOGPS
    logP 5.88 ChemAxon
    logS -5.3 ALOGPS
    pKa (strongest basic) 8.4 ChemAxon
    physiological charge 1 ChemAxon
    hydrogen acceptor count 2 ChemAxon
    hydrogen donor count 0 ChemAxon
    polar surface area 6.48 ChemAxon
    rotatable bond count 6 ChemAxon
    refractivity 119.86 ChemAxon
    polarizability 43.96 ChemAxon
    药物相互作用
    食物相互作用
    Not Available

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