1893-33-0

• 常用中文名：匹泮哌隆
• 常用英文名：Pipamperone
• CAS号：1893-33-0
• 分子式：C₂₁H₃₀FN₃O₂
• 分子量：375.48000
• 相关类别： 信号通路 G 蛋白偶联受体/G 蛋白 5-HT受体
• 发布时间：2018-10-03 22:55:35
• 更新时间：2024-01-09 19:19:57
• Pipamperone (Floropipamide; McN-JR 3345; R 3345) 是 5-HT2A 受体 (pKi=8.2) 和 D4 受体 (pKi=8.0) 的高亲和力拮抗剂。Pipamperone (Floropipamide; McN-JR 3345; R 3345) 是 D2 受体 (pKi=6.7) 的低亲和力拮抗剂。

名称

• 中文名: 酰胺哌啶酮
• 英文名: pipamperone
• 中文别名: 氟丙哌隆
• 英文别名: Dipiperal; piperonil; floropipamide; MCN-JR-3345; Dipiperon; Pipamperone; R 3345; Piperonyl; Floropipamid; Propitan; PIPAMPERONE DIHYDROCHLORIDE APPROX. 99; 1'-[4-(4-fluoro-phenyl)-4-oxo-butyl]-octahydro-[1,4']bipyridinyl-4'-carboxylic acid amide; FPA; 1'-[3-(p-fluorobenzoyl)propyl]-[1,4'-bipiperidine]-4'-carboxamide; Dipiperone

物化性质

• 密度: 1.174g/cm3
• 沸点: 563.7ºC at 760 mmHg
• 熔点: 126°C(lit.)
• 分子式: C₂₁H₃₀FN₃O₂
• 分子量: 375.48000
• 闪点: 294.7ºC
• 精确质量: 375.23200
• PSA: 66.64000
• LogP: 3.17050
• 蒸汽压: 9.88E-13mmHg at 25°C
• 折射率: 1.556
• 储存条件: 室温

生物活性

• 描述: Pipamperone (Floropipamide; McN-JR 3345; R 3345) 是 5-HT2A 受体 (pKi=8.2) 和 D4 受体 (pKi=8.0) 的高亲和力拮抗剂。Pipamperone (Floropipamide; McN-JR 3345; R 3345) 是 D2 受体 (pKi=6.7) 的低亲和力拮抗剂。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 多巴胺受体
  信号通路 >> 神经信号通路 >> 多巴胺受体
  研究领域 >> 神经疾病
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体
  信号通路 >> 神经信号通路 >> 5-HT受体
• 靶点:

  5-HT2A Receptor:8.2 (pKi)

  5-HT2C Receptor:6.9 (pKi)

  5-HT1 Receptor:5.7 (pKi)

  D4 receptor:8.0 (pKi)

  D2 receptor:6.7 (pKi)

  α1 receptor:7.2 (pKi)

• 参考文献:

  [1]. Erik Buntinx, MD, et al. Selective Serotonergic Properties of Low-Dose Pipamperone May Enhance Antidepressant Effect: Preclinical Evidence.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : DW1050000 CHEMICAL NAME : (1,4'-Bipiperidine)-4'-carboxamide, 1'-(3-(p-fluorobenzoyl)propyl)- CAS REGISTRY NUMBER : 1893-33-0 BEILSTEIN REFERENCE NO. : 0496532 LAST UPDATED : 199706 DATA ITEMS CITED : 12 MOLECULAR FORMULA : C21-H30-F-N3-O2 MOLECULAR WEIGHT : 375.54 WISWESSER LINE NOTATION : T6NTJ DVZ A- DT6NTJ A3VR DF 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 : 160 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : ANPBAZ Acta Neurologia et Psychiatrica Belgica. (Brussels, Belgium) V.48-69, 1948-69. For publisher information, see ANUBBR. Volume(issue)/page/year: 61,611,1961 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 160 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : ANPBAZ Acta Neurologia et Psychiatrica Belgica. (Brussels, Belgium) V.48-69, 1948-69. For publisher information, see ANUBBR. Volume(issue)/page/year: 61,611,1961 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 48 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,188,1972 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 490 mg/kg TOXIC EFFECTS : Behavioral - toxic psychosis REFERENCE : PHMGBN Pharmacology: International Journal of Experimental and Clinical Pharmacology. (S. Karger AG, Postfach CH-4009 Basel, Switzerland) V.1- 1968- Volume(issue)/page/year: 15,485,1977 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 160 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,188,1972 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 66 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,188,1972 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Mammal - dog DOSE/DURATION : >40 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 11,932,1961 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Primate - monkey DOSE/DURATION : >20 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 11,932,1961 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Mammal - cat DOSE/DURATION : >10 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 11,932,1961 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 1500 mg/kg SEX/DURATION : female 10-12 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) REFERENCE : TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 28,621,1981 *** REVIEWS *** TOXICOLOGY REVIEW IDPYAK Industrial Pharmacology. (Mount Kisco, NY) V.1-3, 1974-79. Discontinued. Volume(issue)/page/year: 1,203,1974 TOXICOLOGY REVIEW MDCHAG Medicinal Chemistry: A Series of Monographs. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1963- Volume(issue)/page/year: 4(2),199,1967

安全

• 危害码 (欧洲): Xn
• 风险声明 (欧洲): 22
• WGK德国: 1
• 海关编码: 2933399090

合成路线

39633-82-4 3874-54-2 ~45% 1893-33-0

文献：Leyva-Perez, Antonio; Cabrero-Antonino, Jose R.; Rubio-Marques, Paula; Al-Resayes, Saud I.; Corma, Avelino ACS Catalysis, 2014 , vol. 4, # 3 p. 722 - 731

1183278-95-6 ~% 1893-33-0

文献：Leyva-Perez, Antonio; Cabrero-Antonino, Jose R.; Rubio-Marques, Paula; Al-Resayes, Saud I.; Corma, Avelino ACS Catalysis, 2014 , vol. 4, # 3 p. 722 - 731

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39633-82-4 3874-54-2 1183278-95-6
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海关

海关编码	2933399090
中文概述	2933399090. 其他结构含非稠合吡啶环的化合物. 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, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期
Summary	2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%