2746-81-8

• 常用中文名：Fluphenazine enanthate
• 常用英文名：Fluphenazine enanthate
• CAS号：2746-81-8
• 分子式：C₂₉H₃₈F₃N₃O₂S
• 分子量：549.69100
• 相关类别： 研究领域 神经疾病
• 发布时间：2016-03-02 22:50:58
• 更新时间：2024-01-04 09:14:29
• Fluphenazine enanthate 是第一种长效抗精神病药物,用于治疗精神分裂症。

名称

• 中文名: 氟奋乃静庚酸酯
• 英文名: 2-[4-[3-[2-(trifluoromethyl)phenothiazin-10-yl]propyl]piperazin-1-yl]ethyl heptanoate
• 英文别名: Fluphenazine enantate; 2-(4-{3-[2-(trifluoromethyl)-10H-phenothiazin-10-yl]propyl}piperazin-1-yl)ethyl heptanoate; Fluphenazinenanthat; Fluphenanzin-aenanthat; 2-[4-[3-[2-(Trifluoromethyl)phenothiazin-10-yl]propyl]-1-piperazinyl]ethyl heptanoate; Fluphenazin-aenanthsaeureester; 4-<3-<2-Trifluormethyl-phenothiazinyl-(10)>-propyl>-1-(2-hydroxy-ethyl)-piperazin-heptanoat; 1-heptanoyloxy-2-{4-[3-(2-trifluoromethyl-phenothiazin-10-yl)-propyl]-piperazin-1-yl}-ethane; Moditen-retard; Prolixin Enanthate; fluphenazine enanthate; fluphenazine O-enantate; Eutimox; EINECS 220-385-0

物化性质

• 密度: 1.181g/cm3
• 沸点: 629.4ºC at 760mmHg
• 分子式: C₂₉H₃₈F₃N₃O₂S
• 分子量: 549.69100
• 闪点: 334.4ºC
• 精确质量: 549.26400
• PSA: 61.32000
• LogP: 6.77020
• 蒸汽压: 9.41E-16mmHg at 25°C
• 折射率: 1.544

生物活性

• 描述: Fluphenazine enanthate 是第一种长效抗精神病药物,用于治疗精神分裂症。
• 相关类别:
  信号通路 >> 其他 >> 其他
  研究领域 >> 神经疾病
• 体内研究: 氟奋乃静对映体(2,4,8mg/kg；IM)对回避行为的抑制作用分别持续16、23和28天[1]。氟奋乃静(8mg/kg)的饮酒行为在给药后24小时内几乎完全被抑制[1]。氟奋乃嗪(8 mg/kg)在大鼠体内产生短暂的体重损失[1]。动物模型：Wistar品系雄性成年大鼠54只[1]剂量：2、4、8mg/kg给药：中指数(IM)结果：3种剂量的氟哌嗪分别在16、23、28d时对回避行为有明显抑制作用。
• 参考文献:

  [1]. Kuribara H, et al. Effects of fluphenazine enanthate and fluphenazine decanoate on discriminated avoidanceresponse and water drinking behavior in rats. Psychopharmacology (Berl). 1979 Sep;65(1):1-6.

  [2]. Brissos S, et al. The role of long-acting injectable antipsychotics in schizophrenia: a critical appraisal. Ther Adv Psychopharmacol. 2014 Oct;4(5):198-219.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : MJ2450000 CHEMICAL NAME : Heptanoic acid, 2-(4-(3-(2-(trifluoromethyl)phenothiazin-10-yl)propyl )- 1-piperazinyl)ethyl ester CAS REGISTRY NUMBER : 2746-81-8 LAST UPDATED : 199612 DATA ITEMS CITED : 7 MOLECULAR FORMULA : C29-H38-F3-N3-O2-S MOLECULAR WEIGHT : 549.76 WISWESSER LINE NOTATION : T C666 BN ISJ EXFFF B3- AT6N DNTJ D2OV6 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Human DOSE/DURATION : 357 ug/kg TOXIC EFFECTS : Behavioral - muscle weakness REFERENCE : AJPSAO American Journal of Psychiatry. (American Psychiatric Assoc., Circulation Dept., 1400 K St., NW, Washington, DC 20005) V.78- 1921- Volume(issue)/page/year: 119,779,1963 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intramuscular SPECIES OBSERVED : Human DOSE/DURATION : 1633 ug/kg TOXIC EFFECTS : Musculoskeletal - other changes REFERENCE : BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 2,1071,1966 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 300 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: 6,701,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 50 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: 6,701,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 56 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : CSLNX* U.S. Army Armament Research & Development Command, Chemical Systems Laboratory, NIOSH Exchange Chemicals. (Aberdeen Proving Ground, MD 21010) Volume(issue)/page/year: NX#03337 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intramuscular SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 17200 ug/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: 6,701,1982 *** REVIEWS *** TOXICOLOGY REVIEW ABPYBL Advances in Biochemical Psychopharmacology. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) V.1- 1969- Volume(issue)/page/year: 9,301,1974

安全

• 危险品运输编码: UN 3249
• 包装等级: III
• 危险类别: 6.1(b)