盐酸二苯美伦

盐酸二苯美伦用途

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。

盐酸二苯美伦名称

[ CAS 号 ]:
62232-46-6

[ 中文名 ]:
盐酸二苯美伦

[ 英文名 ]:
Bifemelane hydrochloride

[英文别名 ]:

Bifemelan hydrochloride
Bifemelane hydrochloride

盐酸二苯美伦生物活性

[ 描述 ]:

[ 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.

盐酸二苯美伦物理化学性质

[ 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

盐酸二苯美伦毒性和生态

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

盐酸二苯美伦安全信息

[ 海关编码 ]:
2922299090

盐酸二苯美伦海关

[ 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%