1977-11-3

• 常用中文名：Perlapine
• 常用英文名：Perlapine
• CAS号：1977-11-3
• 分子式：C₁₉H₂₁N₃
• 分子量：291.39000
• 相关类别： 信号通路 G 蛋白偶联受体/G 蛋白 由mAChR
• 发布时间：2017-05-20 17:58:53
• 更新时间：2024-01-10 18:05:40
• Perlapine是一种强效毒蕈碱受体(专由设计药物激活的设计受体)激动剂Perlapine对hM3Dq的选择性是hM3受体的10000倍以上[1]。

名称

• 英文名: 6-(4-methylpiperazin-1-yl)-11H-benzo[c][1]benzazepine
• 英文别名: 6-(4-Methyl-1-piperazinyl)morphanthridine; Perlapina [Spanish]; Perlapinum [INN-Latin]; 6-(4-Methyl-1-piperazinyl)-morphanthridin; Hypnodin; AW-14'2333; 6-(4-methyl-piperazin-1-yl)-11H-dibenzo[b,e]azepine; Morphanthridine,6-(4-methyl-1-piperazinyl); Perlapin; Perlapina [INN-Spanish]; MP-11; 6-(4-Methyl-piperazin-1-yl)-morphanthridin; PERLAPINE

物化性质

• 分子式: C₁₉H₂₁N₃
• 分子量: 291.39000
• 精确质量: 291.17400
• PSA: 18.84000
• LogP: 2.22790
• 蒸汽压: 7.74E-08mmHg at 25°C

生物活性

• 描述: Perlapine是一种强效毒蕈碱受体(专由设计药物激活的设计受体)激动剂Perlapine对hM3Dq的选择性是hM3受体的10000倍以上[1]。
• 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
• 参考文献:

  [1]. Chen X, et al. The first structure-activity relationship studies for designer receptors exclusively activated by designer drugs. ACS Chem Neurosci. 2015 Mar 18;6(3):476-84.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : HO2840000 CHEMICAL NAME : 11H-Dibenz(b,e)azepine, 6-(4-methyl-1-piperazinyl)- CAS REGISTRY NUMBER : 1977-11-3 BEILSTEIN REFERENCE NO. : 0434631 LAST UPDATED : 199612 DATA ITEMS CITED : 7 MOLECULAR FORMULA : C19-H21-N3 MOLECULAR WEIGHT : 291.43 WISWESSER LINE NOTATION : T C676 IN BHJ J- AT6N DNTJ D1 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 : 660 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 4,193,1973 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 420 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 4,193,1973 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 60 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 4,193,1973 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 270 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: 6,770,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 250 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 4,193,1973 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 61 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 4,193,1973 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Unreported SPECIES OBSERVED : Rodent - guinea pig DOSE/DURATION : 680 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : MDACAP Medicamentos de Actualidad. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1965- Volume(issue)/page/year: 11,76,1975

合成路线

1211-06-9 ~% 1977-11-3

文献：Sinha, Ashok Kumar; Nizamuddin, S. Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry, 1984 , vol. 23, # 2 p. 165

90-44-8 ~% 1977-11-3

文献：Sinha, Ashok Kumar; Nizamuddin, S. Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry, 1984 , vol. 23, # 2 p. 165

92560-84-4 ~% 1977-11-3

文献：Sinha, Ashok Kumar; Nizamuddin, S. Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry, 1984 , vol. 23, # 2 p. 165

109-01-3 4998-12-3 ~% 1977-11-3

文献：Sinha, Ashok Kumar; Nizamuddin, S. Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry, 1984 , vol. 23, # 2 p. 165

上下游产品

上游产品  4
1211-06-9 90-44-8 92560-84-4 109-01-3
下游产品  0