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比哌立登

比哌立登用途

Biperiden(KL 373)有抗帕金森症活性,是中枢M1胆碱受体阻断剂。

比哌立登名称

[ CAS 号 ]:
514-65-8

[ 中文名 ]:
比哌立登

[ 英文名 ]:
biperiden

[中文别名 ]:

[英文别名 ]:

Biperidene [INN-French]
EINECS 208-184-6
Biperideno
Biperidene
Biperidine
Beperiden
a-5-Norbornen-2-yl-a-phenyl-1-piperidinepropanol
biperiden
UNII:0FRP6G56LD
Akineton

比哌立登生物活性

[ 描述 ]:

Biperiden(KL 373)有抗帕金森症活性,是中枢M1胆碱受体阻断剂。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 由mAChR

信号通路 >> 神经信号通路 >> mAChR

研究领域 >> 神经疾病

[参考文献]

[1]. Pehl C, et al. Effects of two anticholinergic drugs, trospium chloride and biperiden, on motility and evoked potentials of the oesophagus. Aliment Pharmacol Ther. 1998 Oct;12(10)

[2]. Kornhuber J, et al. Identification of novel functional inhibitors of acid sphingomyelinase. PLoS One. 2011;6(8)

[3]. Myhrer T, et al. Antiparkinson drugs used as prophylactics for nerve agents: studies of cognitive side effects in rats. Pharmacol Biochem Behav. 2008 Jun;89(4):633-8.

[相关活性小分子]

比哌立登物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
462.1±40.0 °C at 760 mmHg

[ 熔点 ]:
114ºC

[ 分子式 ]:
C₂₁H₂₉NO

[ 分子量 ]:
311.461

[ 闪点 ]:
224.5±26.0 °C

[ 精确质量 ]:
311.224915

[ PSA ]:
23.47000

[ LogP ]:
4.01

[ 蒸汽压 ]:
0.0±1.2 mmHg at 25°C

[ 折射率 ]:
1.583

[ 储存条件 ]:
通风低温干燥

[ 水溶解性 ]:
25.1 mg/L

比哌立登毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TN3675000

CHEMICAL NAME :: 1-Piperidinepropanol, alpha-5-norbornen-2-yl-alpha-phenyl-

CAS REGISTRY NUMBER :: 514-65-8

BEILSTEIN REFERENCE NO. :: 0290038

LAST UPDATED :: 199612

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C21-H29-N-O

MOLECULAR WEIGHT :: 311.51

WISWESSER LINE NOTATION :: L55 A CUTJ FXQR&2- AT6NTJ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 750 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,636,1982

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 530 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,636,1982

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 161 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,636,1982

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 195 mg/kg

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

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: 128,204,1960

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 56 mg/kg

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

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: 128,204,1960

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 340 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,636,1982

比哌立登安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

[ 海关编码 ]:
2933399090

比哌立登海关

[ 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%