1553-34-0

• 常用中文名：美噻吨盐酸盐
• 常用英文名：Metixene hydrochloride
• CAS号：1553-34-0
• 分子式：C₂₀H₂₄ClNS
• 分子量：345.93
• 相关类别： 信号通路 G 蛋白偶联受体/G 蛋白 由mAChR
• 发布时间：2018-03-14 08:00:00
• 更新时间：2024-01-11 21:47:48
• Metixene hydrochloride 是一种抗胆碱能、抗帕金森剂,能够有效抑制二苯羟乙酸奎宁酯与毒蕈碱受体 (muscarinic receptor) 结合,IC50 和 Kd 值分别为 55 nM 和 15 nM。

名称

• 中文名: 美噻吨盐酸盐
• 英文名: Piperidine,1-methyl-3-(9H-thioxanthen-9-ylmethyl)-, hydrochloride (1:1)
• 英文别名: methypranol; Trimepranol; metipranolol; Turoptin; 1-Methyl-3-thioxanthen-9-ylmethyl-piperidin,Hydrochlorid; Methixenhydrochlorid; metipronalol; Metixene hydrochloride; OptiPranolol; 1-methyl-3-thioxanthen-9-ylmethyl-piperidine,hydrochloride; Disorat; Metipranololum; methixene hydrochloride

物化性质

• 沸点: 419.7ºC at 760 mmHg
• 分子式: C₂₀H₂₄ClNS
• 分子量: 345.93
• 闪点: 207.6ºC
• 精确质量: 345.13200
• PSA: 28.54000
• LogP: 5.75490
• 蒸汽压: 2.99E-07mmHg at 25°C

生物活性

• 描述: Metixene hydrochloride 是一种抗胆碱能、抗帕金森剂,能够有效抑制二苯羟乙酸奎宁酯与毒蕈碱受体 (muscarinic receptor) 结合,IC50 和 Kd 值分别为 55 nM 和 15 nM。
• 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
• 靶点:

  IC50: 55 nM (mAChR)[1] Ki: 15 nM (mAChR)[1]

• 参考文献:

  [1]. Syvälahti EK, et al. Effects of antiparkinsonian drugs on muscarinic receptor binding in rat brain, heart and lung. Pharmacol Toxicol. 1988 Feb;62(2):90-4.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : TN1944000 CHEMICAL NAME : Piperidine, 1-methyl-3-(thioxanthen-9-ylmethyl)-, hydrochloride CAS REGISTRY NUMBER : 1553-34-0 LAST UPDATED : 198812 DATA ITEMS CITED : 8 MOLECULAR FORMULA : C20-H23-N-S.Cl-H MOLECULAR WEIGHT : 345.96 WISWESSER LINE NOTATION : T C666 BS IHJ I1- CT6NTJ A1 &GH 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 : 1460 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: 6,824,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 295 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: 6,824,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 1519 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: 6,824,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 24 mg/kg TOXIC EFFECTS : Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage) Behavioral - convulsions or effect on seizure threshold Behavioral - changes in motor activity (specific assay) 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: 141,331,1963 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 346 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: 6,824,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 108 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: 6,824,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 238 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: 6,824,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 18 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : JPMSAE Journal of Pharmaceutical Sciences. (American Pharmaceutical Assoc., 2215 Constitution Ave., NW, Washington, DC 20037) V.50- 1961- Volume(issue)/page/year: 63,568,1964

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