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苯海索

苯海索用途

三己苯基是一种有效且选择性的M1毒蕈碱受体拮抗剂。三己苯基具有抗胆碱能活性,可用于帕金森综合征或肌张力障碍研究[1][2]。

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苯海索名称

[ CAS 号 ]:
144-11-6

[ 中文名 ]:
苯海索

[ 英文名 ]:
Trihexylphenedyl

[中文别名 ]:

[英文别名 ]:

Parkinane retard
Trihexane
trihexyphenidyle
Artane
1-cyclohexyl-1-phenyl-3-piperidin-1-yl-propan-1-ol
trihexyphenidyl
Benzhexolum
Trihexifenidilo
EINECS 205-614-4
Cyclodol

苯海索生物活性

[ 描述 ]:

三己苯基是一种有效且选择性的M1毒蕈碱受体拮抗剂。三己苯基具有抗胆碱能活性,可用于帕金森综合征或肌张力障碍研究[1][2]。

[ 相关类别 ]:

信号通路 >> 神经信号通路 >> mAChR

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 由mAChR

研究领域 >> 神经疾病

信号通路 >> 神经信号通路 >> 疼痛

[参考文献]

[1]. Giachetti A, et al. Binding and functional profiles of the selective M1 muscarinic receptor antagonists trihexyphenidyl and dicyclomine. Br J Pharmacol. 1986 Sep;89(1):83-90.

[2]. Jilani TN, et al. Trihexyphenidyl. 2022 Feb 27. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2022 Jan–.

苯海索物理化学性质

[ 密度 ]:
1.04g/cm3

[ 沸点 ]:
447.9ºC at 760 mmHg

[ 熔点 ]:
258.5ºC

[ 分子式 ]:
C₂₀H₃₁NO

[ 分子量 ]:
301.46600

[ 闪点 ]:
211ºC

[ 精确质量 ]:
301.24100

[ PSA ]:
23.47000

[ LogP ]:
4.26840

[ 外观性状 ]:
白色固体

[ 蒸汽压 ]:
8.34E-09mmHg at 25°C

[ 折射率 ]:
1.546

[ 储存条件 ]:
室温，密闭，干燥

苯海索毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TN2620000

CHEMICAL NAME :: 1-Piperidinepropanol, alpha-cyclohexyl-alpha-phenyl-

CAS REGISTRY NUMBER :: 144-11-6

BEILSTEIN REFERENCE NO. :: 0088959

LAST UPDATED :: 199612

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C20-H31-N-O

MOLECULAR WEIGHT :: 301.52

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 335 mg/kg

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

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 20,1778,1970

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 150 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified Behavioral - excitement Behavioral - irritability

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 21,1727,1971

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 153 mg/kg

TOXIC EFFECTS :: Behavioral - ataxia Behavioral - muscle contraction or spasticity Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: FATOAO Farmakologiya i Toksikologiya (Moscow). For English translation, see PHTXA6 and RPTOAN. (V/O Mezhdunarodnaya Kniga, 113095 Moscow, USSR) V.2- 1939- Volume(issue)/page/year: 23,8,1960

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 41 mg/kg

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

REFERENCE :: AEPPAE Naunyn-Schmiedeberg's Archiv fuer Experimentelle Pathologie und Pharmakologie. (Berlin, Ger.) V.110-253, 1925-66. For publisher information, see NSAPCC. Volume(issue)/page/year: 226,18,1955

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苯海索安全信息

[ 海关编码 ]:
2933399090

苯海索合成路线

详细合成路线

苯海索上下游产品

苯海索上游产品

苯海索下游产品

苯海索海关

[ 海关编码 ]: 2933399090

[ 中文概述 ]:
2933399090. 其他结构含非稠合吡啶环的化合物. 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, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

苯海索