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盐酸贝那替嗪

盐酸贝那替嗪用途

Benactyzine hydrochloride 是一种丁酰胆碱酯酶 (BChE) 抑制剂,其 Ki 值为 0.010 mM。

盐酸贝那替嗪名称

[ CAS 号 ]:
57-37-4

[ 中文名 ]:
盐酸贝那替嗪

[ 英文名 ]:
Benactyzine hydrochloride

[中文别名 ]:

[英文别名 ]:

β-Diethylaminoethyl benzilate hydrochloride
MFCD00012624
EINECS 200-324-4

盐酸贝那替嗪生物活性

[ 描述 ]:

Benactyzine hydrochloride 是一种丁酰胆碱酯酶 (BChE) 抑制剂,其 Ki 值为 0.010 mM。

[ 相关类别 ]:

信号通路 >> 神经信号通路 >> 疼痛

研究领域 >> 神经疾病

[ 靶点 ]

Ki: 0.010 mM (BChE)[1]

[体外研究]

苯丙嗪盐酸盐和多非洛芬是广泛使用的抗胆碱能药物,它们也是BChE的竞争性抑制剂,Ki值分别为0.010±0.001和0.003±0.000mM。结果表明盐酸苯丙嗪对BChE的抑制作用是纯的或部分竞争性的。通过在固定[BTCh] [1]下绘制v与[Benactyzine]的关系,可以将纯竞争抑制与部分竞争抑制区分开来。

[体内研究]

盐酸苯丙嗪(1 mg/kg)不影响注意力反应。盐酸苯丙嗪增加了探索性运动反应的持续时间,但略微减少了乙酰胆碱引起的唾液分泌。盐酸苯丙嗪和丙嗪对乙酰胆碱引起的EEG癫痫发作没有阻断作用,对情绪反应几乎没有抑制作用。高剂量的丙咪嗪和丙嗪可阻断情绪反应,但盐酸苯丙嗪不能阻止情绪反应。数据表明,丙咪嗪,丙嗪和盐酸苯丙嗪以不同方式影响5-羟色胺的自主神经作用。 Promazine,特别是盐酸Benactyzine,抑制和缩短杏仁内注射5-羟色胺引起的流涎期[2]。

[激酶实验]

使用丁酰硫代胆碱碘化物（BTCh）作为底物，用分光光度计通过分光光度法测量丁酰胆碱酯酶活性。在动力学研究中，通过在5mM 3-（N-吗啉代）丙磺酸（MOPS）缓冲液中使用0.25mM 5,5'-二硫代 - 双（2-硝基苯甲酸）（DTNB）在37℃下测量初始速度。，pH7.5，以及在水中制备的适当浓度的盐酸苯甲嗪和多呋辛胺溶液，作为在0.5mL最终体积的测定混合物中0.25-2.0mM BTCh的BTCh浓度的函数（0.5mL测定混合物含有1.56mg纯化的酶）。分析一式两份进行，活动测量最多90秒[1]。

[动物实验]

在自由行为情况下，在体重为1.8至4kg的36只性别的猫中进行实验。实验按以下顺序进行：首次将微量注射乙酰胆碱和/或5-羟色胺和/或去甲肾上腺素（200μg）进入杏仁核后，记录行为，自主反应和脑电图的变化，持续10年。然后肌肉内注射丙咪嗪和/或盐酸苯丙嗪和/或丙嗪和/或盐水（在对照实验中）。在肌肉注射药物和/或生理盐水后，在45天雨中进行第二次神经激素（200μg）微量注射到杏仁核中，并且通过第一次微注射诱导效果与前一次相比[2] 。

[参考文献]

[1]. Bodur E, et al. Inhibition effects of benactyzine and drofenine on human serum butyrylcholinesterase. Arch Biochem Biophys. 2001 Feb 1;386(1):25-9.

[2]. Allikmets LH, et al. Dissimilar influences of imipramine, benactyzine and promazine on effects of micro-injections ofnoradrenaline, acetylcholine and serotonin into the amygdala in the cat. Psychopharmacologia. 1969;15(5):392-403.

[相关活性小分子]

盐酸贝那替嗪物理化学性质

[ 密度 ]:
1.115g/cm3

[ 沸点 ]:
409.3ºC at 760mmHg

[ 熔点 ]:
177-179 °C(lit.)

[ 分子式 ]:
C₂₀H₂₆ClNO₃

[ 分子量 ]:
363.878

[ 闪点 ]:
201.4ºC

[ 精确质量 ]:
363.160126

[ PSA ]:
49.77000

[ LogP ]:
3.60950

[ 储存条件 ]:
通风低温干燥,与库房食品原料分开存放

盐酸贝那替嗪MSDS

详细MSDS(安全技术说明书)

盐酸贝那替嗪毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DD2800000

CHEMICAL NAME :: Benzilic acid, 2-(diethylamino)ethyl ester, hydrochloride

CAS REGISTRY NUMBER :: 57-37-4

LAST UPDATED :: 199706

DATA ITEMS CITED :: 13

MOLECULAR FORMULA :: C20-H25-N-O3.Cl-H

MOLECULAR WEIGHT :: 363.92

WISWESSER LINE NOTATION :: QXR&R&VO2N2&2 &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human

DOSE/DURATION :: 14 ug/kg

TOXIC EFFECTS :: Behavioral - toxic psychosis

REFERENCE :: 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,363,1972

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 184 mg/kg

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

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 1,42,1959

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 100 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - excitement Lungs, Thorax, or Respiration - respiratory stimulation

REFERENCE :: APTOA6 Acta Pharmacologica et Toxicologica. (Copenhagen, Denmark) V.1-59, 1945-86. For publisher information, see PHTOEH Volume(issue)/page/year: 11,405,1955

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 160 mg/kg

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

REFERENCE :: 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,363,1972

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 76 mg/kg

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

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 74,274,1942

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 250 mg/kg

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

REFERENCE :: 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,363,1972

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 14300 ug/kg

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

REFERENCE :: 85JCAE "Prehled Prumyslove Toxikologie; Organicke Latky," Marhold, J., Prague, Czechoslovakia, Avicenum, 1986 Volume(issue)/page/year: -,673,1986

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intradermal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 350 mg/kg

TOXIC EFFECTS :: Behavioral - excitement Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 59,149,1938

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 100 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - excitement Lungs, Thorax, or Respiration - respiratory stimulation

REFERENCE :: APTOA6 Acta Pharmacologica et Toxicologica. (Copenhagen, Denmark) V.1-59, 1945-86. For publisher information, see PHTOEH Volume(issue)/page/year: 11,405,1955

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 15 mg/kg

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

REFERENCE :: 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,363,1972

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 100 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - excitement Lungs, Thorax, or Respiration - respiratory stimulation

REFERENCE :: APTOA6 Acta Pharmacologica et Toxicologica. (Copenhagen, Denmark) V.1-59, 1945-86. For publisher information, see PHTOEH Volume(issue)/page/year: 11,405,1955 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 500 ug/kg

SEX/DURATION :: male 1 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - mating performance (e.g. # sperm positive females per # females mated; # copulations per # estrus cycles)

REFERENCE :: PSYPAG Psychopharmacologia (Berlin). (Berlin, Ger.) V.1-46, 1959-76. For publisher information, see PSCHDL. Volume(issue)/page/year: 10,44,1966

盐酸贝那替嗪安全信息

[ 危害码 (欧洲) ]:
T:Toxic;

[ 风险声明 (欧洲) ]:
R23/24/25

[ 安全声明 (欧洲) ]:
S36/37/39-S45

[ 危险品运输编码 ]:
UN 2811 6.1/PG 3

[ WGK德国 ]:
3

[ RTECS号 ]:
DD2800000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

盐酸贝那替嗪制备

由二苯乙醇酸与1-氯-2二乙氨基乙烷反应得到。将甲苯、二苯乙醇酸和1-氯-2-二乙氨基乙烷在反应锅内加热回流3h，冷却结晶，甩滤得到的粗品经精制即为该品。