5169-78-8

• 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]。

名称

• 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

物化性质

• 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

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.

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

安全

• 海关编码: 2934999090

合成路线

5166-68-7 ~% 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 1690-72-8 ~% 5169-78-8

文献：Kawazu; Kanno; Saito; Tamaki Journal of medicinal chemistry, 1972 , vol. 15, # 9 p. 914 - 918

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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%