62232-46-6

• 常用中文名：盐酸二苯美伦
• 常用英文名：Bifemelane hydrochloride
• CAS号：62232-46-6
• 分子式：C₁₈H₂₄ClNO
• 分子量：305.84200
• 相关类别： 信号通路 神经信号通路 单胺氧化酶
• 发布时间：2018-09-03 19:14:30
• 更新时间：2024-01-07 23:03:51
• Bifemelane hydrochloride 是一种有效,选择性和竞争性的单胺氧化酶 A (MAO-A) 抑制剂,Ki 值为 4.20 μM,它也非竞争性地抑制 MAO-B,Ki 为 46.0 μM。Bifemelane hydrochloride 具有很强的抗抑郁活性,可用于研究与脑血管疾病有关的认知和情绪障碍。

名称

• 中文名: 盐酸二苯美伦
• 英文名: Bifemelane HCl
• 英文别名: Bifemelan hydrochloride; Bifemelane hydrochloride

物化性质

• 沸点: 395.4ºC at 760 mmHg
• 熔点: 117-121°C
• 分子式: C₁₈H₂₄ClNO
• 分子量: 305.84200
• 闪点: 169.2ºC
• 精确质量: 305.15500
• PSA: 21.26000
• LogP: 4.84870
• 储存条件: 2-8°C

生物活性

• 描述: Bifemelane hydrochloride 是一种有效,选择性和竞争性的单胺氧化酶 A (MAO-A) 抑制剂,Ki 值为 4.20 μM,它也非竞争性地抑制 MAO-B,Ki 为 46.0 μM。Bifemelane hydrochloride 具有很强的抗抑郁活性,可用于研究与脑血管疾病有关的认知和情绪障碍。
• 相关类别:
  信号通路 >> 神经信号通路 >> 单胺氧化酶
  研究领域 >> 神经疾病
• 靶点:

  MAO-A:4.2 μM (Ki)

  MAO-B:46 μM (Ki)

• 体外研究: 联苯胺对MAO-A的抑制作用呈剂量依赖性,人脑突触体和肝线粒体的Kis分别为4.2±0.2和14.1±0.7μM[1]。联苯胺对MAO-B活性具有剂量依赖性抑制作用,其在人脑突触体和人肝线粒体中的Kis分别为46.0±3.6和65.2±7.0μM[1]。
• 体内研究: 联苯胺(20-80毫克/千克；静脉注射)剂量依赖性地降低了野外试验中的勘探活性[3]。联苯胺(20-80 mg/kg；i.p.)可减少强迫游泳试验中的静止时间,但其剂量依赖性不明显,已经达到20 mg/kg的上限[3]。动物模型：用利血平诱导雄性大鼠(230～270g)低温[3]剂量：20、40、80mg/kg给药：单次静脉注射。结果：利血平诱导的体温降低最多10℃。
• 参考文献:

  [1]. Naoi M, et, al. 4-(O-benzylphenoxy)-N-methylbutylamine (bifemelane) and other 4-(O-benzylphenoxy)-N-methylalkylamines as new inhibitors of type A and B monoamine oxidase. J Neurochem. 1988 Jan; 50(1): 243-7.

  [2]. Fasipe OJ, et, al. The emergence of new antidepressants for clinical use: Agomelatine paradox versus other novel agents. IBRO Rep. 2019 Jan 9; 6:95-110.

  [3]. Moryl E, et, al. Potential antidepressive properties of amantadine, memantine and bifemelane. Pharmacol Toxicol. 1993 Jun; 72(6): 394-7.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : EJ4091000 CHEMICAL NAME : 1-Butanamine, N-methyl-4-(2-(phenylmethyl)phenoxy)-, hydrochloride CAS REGISTRY NUMBER : 62232-46-6 LAST UPDATED : 199409 DATA ITEMS CITED : 12 MOLECULAR FORMULA : C18-H23-N-O.Cl-H MOLECULAR WEIGHT : 305.88 WISWESSER LINE NOTATION : 1M4OR B1R &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 : 1080 mg/kg TOXIC EFFECTS : Behavioral - tremor Behavioral - convulsions or effect on seizure threshold Behavioral - muscle weakness REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 31,1278,1981 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 130 mg/kg TOXIC EFFECTS : Behavioral - tremor Behavioral - convulsions or effect on seizure threshold Behavioral - muscle weakness REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 31,1278,1981 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 513 mg/kg TOXIC EFFECTS : Sense Organs and Special Senses (Eye) - lacrimation Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 31,587,1986 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 40400 ug/kg TOXIC EFFECTS : Sense Organs and Special Senses (Eye) - lacrimation Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 31,587,1986 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 400 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold REFERENCE : CCCCAK Collection of Czechoslovak Chemical Communications. (Academic Press Inc. Ltd., 24-28 Oval Rd., London NW1 7DX, UK) V.1- 1929- Volume(issue)/page/year: 53,1307,1988 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 105 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 16,1181,1988 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 313 mg/kg TOXIC EFFECTS : Sense Organs and Special Senses (Eye) - lacrimation Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 31,587,1986 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 35300 ug/kg TOXIC EFFECTS : Sense Organs and Special Senses (Eye) - lacrimation Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 31,587,1986 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 151 mg/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Behavioral - food intake (animal) Gastrointestinal - changes in structure or function of salivary glands REFERENCE : SHNSAS Shinryo to Shinyaku. Medical Consultation and New Remedies. (Iji Shuppan Sha, 1-2-8 Shinkawa, Chuo-Ku, Tokyo 104, Japan) V.1- 1964- Volume(issue)/page/year: 23,43,1986 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 11375 mg/kg/13W-C TOXIC EFFECTS : Liver - fatty liver degeneration Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Nutritional and Gross Metabolic - weight loss or decreased weight gain REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 31,587,1986 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 9100 mg/kg/52W-C TOXIC EFFECTS : Liver - fatty liver degeneration Kidney, Ureter, Bladder - other changes in urine composition Blood - changes in erythrocyte (RBC) count REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 31,601,1986 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 24 gm/kg/52W-I TOXIC EFFECTS : Liver - changes in liver weight Blood - changes in leukocyte (WBC) count Related to Chronic Data - death REFERENCE : SHNSAS Shinryo to Shinyaku. Medical Consultation and New Remedies. (Iji Shuppan Sha, 1-2-8 Shinkawa, Chuo-Ku, Tokyo 104, Japan) V.1- 1964- Volume(issue)/page/year: 23,57,1986

安全

• 海关编码: 2922299090

海关

海关编码	2922299090
中文概述	2922299090. 其他氨基(萘酚、酚)及醚、酯〔包括它们的盐, 但含有一种以上含氧基的除外〕. 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:30.0%
申报要素	品名, 成分含量, 用途, 乙醇胺及其盐应报明色度, 乙醇胺及其盐应报明包装
Summary	2922299090. other amino-naphthols and other amino-phenols, other than those containing more than one kind of oxygen function, their ethers and esters; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%