替培啶

替培啶用途

替匹定可逆抑制多巴胺(DA)D2受体介导的GIRK电流(IDA(GIRK)),IC50为7.0μM。替匹定随后激活VTA多巴胺神经元[1]。替匹定是一种非麻醉性镇咳药,具有抗抑郁作用[2]。

替培啶名称

[ CAS 号 ]:
5169-78-8

[ 中文名 ]:
替培啶

[ 英文名 ]:
tipepidine

[英文别名 ]:

替培啶生物活性

[ 描述 ]:

替匹定可逆抑制多巴胺(DA)D2受体介导的GIRK电流(IDA(GIRK)),IC50为7.0μM。替匹定随后激活VTA多巴胺神经元[1]。替匹定是一种非麻醉性镇咳药,具有抗抑郁作用[2]。

[ 相关类别 ]:

研究领域 >> 神经疾病
信号通路 >> 跨膜转运 >> 钾通道

[ 靶点 ]

IC50: 7.0 μM (dopamine D2 receptor)[1]


[体内研究]

替匹定(i.p.；10-40 mg/kg；0.5-23小时)可显著缩短ACTH治疗大鼠在强迫游泳试验中的不动时间。替匹定(i.p.；40 mg/kg)可提高ACTH治疗大鼠伏隔核(NAc)细胞外多巴胺水平[2]。动物模型：雄性Wistar大鼠,体重150-240 g(5-7周龄)[2]剂量：10、20和40 mg/kg。管理：I.p。；0.5,5,23小时。结果：ACTH可缩短大鼠强迫游泳实验中的不动时间。

[参考文献]

[1]. Hamasaki R, et al. Tipepidine activates VTA dopamine neuron via inhibiting dopamine D₂ receptor-mediated inward rectifying K⁺ current. Neuroscience. 2013 Nov 12;252:24-34.

[2]. Kawaura K, et al. Tipepidine, a non-narcotic antitussive, exerts an antidepressant-like effect in the forced swimming test in adrenocorticotropic hormone-treated rats. Behav Brain Res. 2016 Apr 1;302:269-78.

替培啶物理化学性质

[ 密度 ]:
1.1947 (rough estimate)

[ 沸点 ]:
bp4-5 178-184°

[ 熔点 ]:
64-65°

[ 分子式 ]:
C15H17NS2

[ 分子量 ]:
275.43200

[ 精确质量 ]:
275.08000

[ PSA ]:
59.72000

[ LogP ]:
4.27500

[ 折射率 ]:
1.5300 (estimate)

[ 储存条件 ]:
库房通风低温干燥,与氧化剂、酸类分开存放

替培啶毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
TM7870000
CHEMICAL NAME :
Piperidine, 3-(di-2-thienylmethylene)-1-methyl-
CAS REGISTRY NUMBER :
5169-78-8
BEILSTEIN REFERENCE NO. :
0212554
LAST UPDATED :
199612
DATA ITEMS CITED :
6
MOLECULAR FORMULA :
C15-H17-N-S2
MOLECULAR WEIGHT :
275.45
WISWESSER LINE NOTATION :
T6N CYTJ A1 CUY- BT5SJ&- BT5SJ

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 :
867 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
85KYAH "Merck Index; an Encyclopedia of Chemicals, Drugs, and Biologicals", 11th ed., Rahway, NJ 07065, Merck & Co., Inc. 1989 Volume(issue)/page/year: 11,1490,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
294 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
85KYAH "Merck Index; an Encyclopedia of Chemicals, Drugs, and Biologicals", 11th ed., Rahway, NJ 07065, Merck & Co., Inc. 1989 Volume(issue)/page/year: 11,1490,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
222 mg/kg
TOXIC EFFECTS :
Brain and Coverings - recordings from specific areas of CNS Behavioral - excitement Lungs, Thorax, or Respiration - other changes
REFERENCE :
CPBTAL Chemical and Pharmaceutical Bulletin. (Japan Pub. Trading Co., USA, 1255 Howard St., San Francisco, CA 94103) V.6- 1958- Volume(issue)/page/year: 7,372,1959
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
55 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
PCJOAU Pharmaceutical Chemistry Journal (English Translation). Translation of KHFZAN. (Plenum Pub. Corp., 233 Spring St., New York, NY 10013) No.1- 1967- Volume(issue)/page/year: 10,1482,1976
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
308 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
85KYAH "Merck Index; an Encyclopedia of Chemicals, Drugs, and Biologicals", 11th ed., Rahway, NJ 07065, Merck & Co., Inc. 1989 Volume(issue)/page/year: 11,1490,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
44 mg/kg
TOXIC EFFECTS :
Behavioral - food intake (animal) Behavioral - muscle weakness Lungs, Thorax, or Respiration - respiratory stimulation
REFERENCE :
CPBTAL Chemical and Pharmaceutical Bulletin. (Japan Pub. Trading Co., USA, 1255 Howard St., San Francisco, CA 94103) V.6- 1958- Volume(issue)/page/year: 7,372,1959

替培啶安全信息

[ 海关编码 ]:
2934999090

替培啶合成路线

详细合成路线

替培啶上下游产品

替培啶上游产品

替培啶下游产品

替培啶海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 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

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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