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相关CAS号：
5169-78-8 31139-87-4
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5169-78-8

5169-78-8结构式
5169-78-8结构式
  • 常用中文名：替培啶
  • 常用英文名：tipepidine
  • CAS号：5169-78-8
  • 分子式：C15H17NS2
  • 分子量：275.43200
  • 相关类别： 原料药 呼吸系统用药 镇咳药
  • 发布时间：2018-03-18 08:00:00
  • 更新时间：2024-01-11 12:24:31
  • 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]。

化源商城直购

中文名 替培啶
英文名 3-(dithiophen-2-ylmethylidene)-1-methylpiperidine
英文别名 3-(di-thiophen-2-yl-methylene)-1-methyl-piperidine
Bitiodin
Asverin
(1-Methyl-3-piperidylidene)di(2-thienyl)methane
Tipepidine [INN:DCF]
Tipepidine
3-(Di-[2]thienyl-methylen)-1-methyl-piperidin
Tipepidina [INN-Spanish]
Tipedine
Tipepidinum [INN-Latin]
(1-Methyl-3-piperidyliden)di-2-thienylmethan-embonat
CR/662
AT 327
3-(di-[2]thienyl-methylene)-1-methyl-piperidine
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
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.
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

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

海关编码 2934999090
5166-68-7结构式

5166-68-7

~%

5169-78-8结构式

5169-78-8
文献：Okumura et al. Ann. Rep. Tanabe pharm. Res.Chem.Abstr., 1958 , vol. 3, # 2 p. 30,32 Ann. Rep. Tanabe pharm. Res.Chem.Abstr., 1959 , p. 10214
1003-09-4结构式

1003-09-4
1690-72-8结构式

1690-72-8

~%

5169-78-8结构式

5169-78-8
文献：Kawazu; Kanno; Saito; Tamaki Journal of medicinal chemistry, 1972 , vol. 15, # 9 p. 914 - 918
上游产品  3

下游产品  0

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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