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苯氧苄胺

苯氧苄胺用途

Phenoxybenzamine hydrochloride 是具有选择行的 α-adrenoceptor 和 calmodulin 的抑制剂,是一种常用的抗高血压药。

苯氧苄胺名称

[ CAS 号 ]:
63-92-3

[ 中文名 ]:
盐酸酚苄明

[ 英文名 ]:
Phenoxybenzamine HCl

[中文别名 ]:

[英文别名 ]:

MFCD00599580
Bensylyte Hydrochloride
Dibenyline
Phenoxybenzamine HCl
(±)-Phenoxybenzamine Hydrochloride
Bensylyt Hydrochloride
Phenoxybenzamine Hydrochloride
EINECS 200-569-7
Dibenzyran
Phenoxybenzamine (hydrochloride)

苯氧苄胺生物活性

[ 描述 ]:

Phenoxybenzamine hydrochloride 是具有选择行的 α-adrenoceptor 和 calmodulin 的抑制剂,是一种常用的抗高血压药。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 肾上腺素能受体

研究领域 >> 心血管疾病

[体外研究]

由苯氧基苯甲胺盐酸盐阻断[3H]育亨宾的IC50(100 nM)明显低于盐酸苯氧苄胺对环磷酸腺苷累积影响的相应逆转IC50(550 nM)[1]。苯氧苄胺盐酸盐(50 nM)与苯氧基苯甲胺盐酸胺(1000 nM)相结合,与在内皮完整主动脉中单独使用苯氧基苯甲胺盐酸盐(50 nM)预处理相比,增强了苯氧苄胺盐酸盐去氧肾上腺素诱导的收缩。与单独的苯氧基苯甲胺盐酸盐(50nM)相比,用右美托咪定(300或1000nM)和苯氧基苯甲胺盐酸盐(50nM)或苯氧基苯甲胺盐酸盐(1000nM)和苯氧基苯甲胺盐酸盐(50nM)的联合处理增强了苯氧基苯甲胺盐酸盐酰胺诱导的收缩。此外,与右美托咪定(1000 nM)和盐酸苯氧苄胺联合处理相比,与苯氧基苯甲胺盐酸胺和盐酸苯氧基苯甲胺的联合处理增强了苯氧基苯甲胺盐酸去氧肾上腺素诱导的收缩。与低浓度右美托咪定(300 nM)和盐酸苯氧苄胺联合治疗相比,高浓度右美托咪定(1000 nM)和盐酸苯氧苄胺联合治疗可增强苯氧苄胺盐酸盐去氧肾上腺素诱导的收缩[2]。苯氧苄胺盐酸盐(0.1-100μM)抑制胶质瘤增殖,迁移和侵袭,并抑制肿瘤发生能力。苯氧基苯甲胺盐酸盐也抑制胶质瘤干细胞样细胞的自我更新。 Phenoxybenzamine hydrochloride激活LINGO-1并抑制TrkB-Akt通路[3]。苯氧苄胺盐酸盐(0.1μM-1 mM)可保留CA1,CA3和齿状回内的原代神经元,并产生强大的神经保护作用,并在分娩后2,4和8小时分娩时防止海马区域内OGD神经元死亡-OGD为100μM[4]。

[体内研究]

苯氧苄胺盐酸盐(20 nM,sc)有效抑制小鼠胶质瘤细胞的肿瘤发生,苯氧苄胺盐酸盐-U87MG异种移植物的细胞密度显着降低[3]。苯氧苄胺盐酸盐(1 mg/kg,iv)处理的大鼠在NSS和足部缺陷评分方面显示出显着改善[4]。

[细胞实验]

细胞计数后，将1×3细胞植入96孔板中的100μL补充有10％FBS的DMEM中。将10微升（总体积的10％）WST-1（水溶性四唑鎓）加入细胞中并在37℃下孵育30分钟，然后进行比色测定，以450nm激发和630nm发射，间隔24小时，直至96小时。。计算平均荧光值，并使用标准曲线确定细胞数。

[动物实验]

将U87MG细胞以每侧2.0×3 /200μL的剂量皮下注射到裸鼠的两侧。注射后8天，在小鼠的两侧肉眼观察到肿瘤生长。然后，以2天的间隔将20nM苯氧基苯甲胺盐酸盐皮下注射到右侧，并将溶剂DMSO用作对照。通过测量长度（a）和宽度（b）确定肿瘤体积（V）并使用以下等式计算：V =（ab）2/2。

[参考文献]

[1]. Lenox, R.H., et al, Alpha 2-adrenergic receptor-mediated regulation of adenylate cyclase in the intact human platelet. Evidence for a receptor reserve. Mol Pharmacol, 1985. 27(1): p. 1-9.

[2]. Byon HJ, et al. Dexmedetomidine Inhibits Phenylephrine-induced Contractions via Alpha-1 Adrenoceptor Blockade and Nitric Oxide Release in Isolated Rat Aortae. Int J Med Sci. 2017 Feb 7;14(2):143-149.

[3]. Lin XB, et al. Anti-tumor activity of phenoxybenzamine hydrochloride on malignant glioma cells. Tumour Biol. 2016 Mar;37(3):2901-8.

[4]. Rau TF, et al. Phenoxybenzamine is neuroprotective in a rat model of severe traumatic brain injury. Int J Mol Sci. 2014 Jan 20;15(1):1402-17.

[相关活性小分子]

苯氧苄胺物理化学性质

[ 沸点 ]:
381.5ºC at 760 mmHg

[ 熔点 ]:
137.5°C

[ 分子式 ]:
C₁₈H₂₃Cl₂NO

[ 分子量 ]:
340.287

[ 闪点 ]:
184.5ºC

[ 精确质量 ]:
339.115662

[ PSA ]:
12.47000

[ LogP ]:
4.99690

[ 外观性状 ]:
白色结晶粉末

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
H2O: slightly soluble | <0.01 g/100 mL at 18.5 ºC

苯氧苄胺MSDS

详细MSDS(安全技术说明书)

苯氧苄胺毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DP3750000

CHEMICAL NAME :: Benzylamine, N-(2-chloroethyl)-N-(1-methyl-2-phenoxyethyl)-, hydrochloride

CAS REGISTRY NUMBER :: 63-92-3

LAST UPDATED :: 199601

DATA ITEMS CITED :: 20

MOLECULAR FORMULA :: C18-H22-Cl-N-O.Cl-H

MOLECULAR WEIGHT :: 340.32

WISWESSER LINE NOTATION :: G2N1R&Y1&1OR &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 7143 ug/kg/5D-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis)

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 800 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 900 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 99 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 105 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 63750 ug/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea Lungs, Thorax, or Respiration - other changes

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 780 mg/kg/1Y-I

TOXIC EFFECTS :: Tumorigenic - Carcinogenic by RTECS criteria Gastrointestinal - tumors

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 3900 mg/kg/52W-I

TOXIC EFFECTS :: Tumorigenic - Carcinogenic by RTECS criteria Gastrointestinal - tumors

TYPE OF TEST :: TD - Toxic dose (other than lowest)

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1560 mg/kg/1Y-I

TOXIC EFFECTS :: Tumorigenic - Carcinogenic by RTECS criteria Gastrointestinal - tumors

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 12 mg/kg

SEX/DURATION :: female 5-12 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Parenteral

DOSE :: 24500 ug/kg

SEX/DURATION :: male 35 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count) Reproductive - Paternal Effects - testes, epididymis, sperm duct Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Parenteral

DOSE :: 24500 ug/kg

SEX/DURATION :: male 35 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - male fertility index (e.g. # males impregnating females per # males exposed to fertile nonpregnant females)

MUTATION DATA

TYPE OF TEST :: Mutation in microorganisms

TEST SYSTEM :: Bacteria - Salmonella typhimurium

DOSE/DURATION :: 3 ug/plate

REFERENCE :: EMMUEG Environmental and Molecular Mutagenesis. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.10- 1987- Volume(issue)/page/year: 11(Suppl 12),1,1988 *** REVIEWS *** IARC Cancer Review:Animal Sufficient Evidence IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 24,185,1980 IARC Cancer Review:Human No Adequate Data IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 24,185,1980 IARC Cancer Review:Group 2B IMSUDL IARC Monographs, Supplement. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) No.1- 1979- Volume(issue)/page/year: 7,56,1987 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5625 No. of Facilities: 44 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 796 (estimated) No. of Female Employees: 406 (estimated)

苯氧苄胺安全信息

[ 符号 ]:

GHS07, GHS08

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H351

[ 警示性声明 ]:
P301 + P312 + P330

[ 个人防护装备 ]:
Eyeshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
Xn:Harmful;

[ 风险声明 (欧洲) ]:
R22;R40

[ 安全声明 (欧洲) ]:
S22-S36/37/39-S45

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
DP3750000

[ 海关编码 ]:
2922299090

苯氧苄胺海关

[ 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%

苯氧苄胺文献

Neurotransmitter-mediated anxiogenic action of PACAP-38 in rats.

Behav. Brain Res. 281 , 333-8, (2015)

The action of PACAP-38 was studied by measuring the anxiogenic-anxiolytic behavior of rats in an elevated plus maze. PACAP-38 was administered into the lateral brain ventricle and the behavior of the ...

Quantitative high-throughput identification of drugs as modulators of human constitutive androstane receptor.

Sci. Rep. 5 , 10405, (2015)

The constitutive androstane receptor (CAR, NR1I3) plays a key role in governing the transcription of numerous hepatic genes that involve xenobiotic metabolism/clearance, energy homeostasis, and cell p...

Targeting the chromosome partitioning protein ParA in tuberculosis drug discovery.

J. Antimicrob. Chemother. 65(11) , 2347-58, (2010)

To identify inhibitors of the essential chromosome partitioning protein ParA that are active against Mycobacterium tuberculosis.Antisense expression of the parA orthologue MSMEG_6939 was induced on th...

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