氰美马嗪

氰美马嗪用途

Cyamemazine 是一种抗精神病药,其中含有吩噻嗪发色团,通常被用作抗焦虑药。Cyamemazine 是具有抗精神病活性的有效的 5-HT3 (Ki 为 12 nM), 5-HT2A (Ki 为 1.5 nM) 和 5-HT2C (Ki 为 75 nM) 受体拮抗剂。

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氰美马嗪名称

[ CAS 号 ]:
3546-03-0

[ 中文名 ]:
氰美马嗪

[ 英文名 ]:
Cyamemazine

[英文别名 ]:

Kyamepromazin
Kyamepromazine
7204 R.E.
Ciamatil
Cyamemazine
Tercian

氰美马嗪生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 神经疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体

信号通路 >> 神经信号通路 >> 5-HT受体

[ 靶点 ]

5-HT2A Receptor:1.5 nM (Ki)

5-HT2C Receptor:12 nM (Ki)

5-HT3 Receptor:75 nM (Ki)

[体外研究]

Cyamemazine对多巴胺受体有很高的亲和力,这与它的抗精神病活性是一致的。Cyamemazine对毒蕈碱受体的拮抗活性与其对M1(Ki=13nm)、M2(Ki=42nm)、M3(Ki=321nm)、M4(Ki=12nm)和M5(Ki=35nm)受体的亲和力一致[1]。

[体内研究]

在离体豚鼠回肠5-HT3依赖性收缩和大鼠心动过缓反应中,在大鼠脑膜5-HT2C依赖性磷脂酶C刺激中,在离体大鼠主动脉环和离体豚鼠气管5-HT2A依赖性收缩中,Cyamemazine作为5-HT3、5-HT2C和5-HT2A受体的拮抗剂。CyimeMa嗪拮抗5-HT3和5-HT2C受体,并且这种效应部分地参与了其在焦虑症中的治疗活性。急性给药小剂量的Cyamemazine可降低大鼠纹状体细胞外多巴胺和代谢物浓度[1]。

[参考文献]

[1]. Bourin M, et al. Preclinical and clinical pharmacology of cyamemazine: anxiolytic effects and prevention of alcohol and benzodiazepine withdrawal syndrome. CNS Drug Rev. 2004 Fall;10(3):219-29.

[2]. Vendrell-Criado V, et al. Photobehavior of the antipsychotic drug cyamemazine in a supramolecular gel protective environment. J Photochem Photobiol B. 2020 Jan;202:111686.

氰美马嗪物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
479.0±45.0 °C at 760 mmHg

[ 分子式 ]:
C₁₉H₂₁N₃S

[ 分子量 ]:
323.455

[ 闪点 ]:
243.5±28.7 °C

[ 精确质量 ]:
323.145630

[ PSA ]:
55.57000

[ LogP ]:
4.62

[ 蒸汽压 ]:
0.0±1.2 mmHg at 25°C

[ 折射率 ]:
1.655

[ 储存条件 ]:
2-8°C，密封，干燥

氰美马嗪MSDS

详细MSDS(安全技术说明书)

氰美马嗪毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: SN6950000

CHEMICAL NAME :: Phenothiazine-2-carbonitrile, 10-(3-(dimethylamino)-2-methylpropyl)-

CAS REGISTRY NUMBER :: 3546-03-0

BEILSTEIN REFERENCE NO. :: 0093261

LAST UPDATED :: 199703

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C19-H21-N3-S

MOLECULAR WEIGHT :: 323.49

WISWESSER LINE NOTATION :: T C666 BN ISJ B1Y1&1N1&1 ECN

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: Standard Draize test

ROUTE OF EXPOSURE :: Administration into the eye

SPECIES OBSERVED :: Rodent - rabbit

REFERENCE :: FCTOD7 Food and Chemical Toxicology. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.20- 1982- Volume(issue)/page/year: 20,573,1982

TYPE OF TEST :: Rinsed with water

ROUTE OF EXPOSURE :: Administration into the eye

SPECIES OBSERVED :: Rodent - rabbit

REFERENCE :: FCTOD7 Food and Chemical Toxicology. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.20- 1982- Volume(issue)/page/year: 20,573,1982 ** ACUTE TOXICITY DATA **

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 107 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JATOD3 Journal of Analytical Toxicology. (Preston Pub. Inc., POB 48312, Niles, IL 60648) V.1- 1977- Volume(issue)/page/year: 17,386,1993

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氰美马嗪安全信息

[ 符号 ]:

GHS09

[ 信号词 ]:
Warning

[ 危害声明 ]:
H410

[ 警示性声明 ]:
P273-P501

[ 危害码 (欧洲) ]:
Xi

[ 危险品运输编码 ]:
UN 3077 9 / PGIII

[ 海关编码 ]:
2934300000

氰美马嗪合成路线

详细合成路线

氰美马嗪上下游产品

氰美马嗪上游产品

氰美马嗪下游产品

氰美马嗪海关

[ 海关编码 ]: 2934300000

[ 中文概述 ]:
2934300000. 含一个吩噻嗪环系的化合物(吩噻嗪环系不论是否氢化,化合物未经进一步稠合的 ). 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2934300000. other compounds containing in the structure a phenothiazine ring-system (whether or not hydrogenated), not further fused. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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