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1-甲基-4-苯基-1,2,3,6-四氢吡啶盐酸盐

1-甲基-4-苯基-1,2,3,6-四氢吡啶盐酸盐用途

MPTP hydrochloride是可渗透血脑屏障的多巴胺神经毒素,能诱导帕金森综合症。

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1-甲基-4-苯基-1,2,3,6-四氢吡啶盐酸盐名称

[ CAS 号 ]:
23007-85-4

[ 中文名 ]:
1-甲基-4-苯基-1,2,3,6-四氢吡啶盐酸盐

[ 英文名 ]:
0MPTP hydrochloride

[中文别名 ]:

[英文别名 ]:

MPTP Hydrochloride
MPTP (hydrochloride)

1-甲基-4-苯基-1,2,3,6-四氢吡啶盐酸盐生物活性

[ 描述 ]:

MPTP hydrochloride是可渗透血脑屏障的多巴胺神经毒素,能诱导帕金森综合症。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 神经疾病

[体外研究]

用50mM 4-苯基吡啶预处理,使小鼠膈神经-膈肌中MPTP(50％抑制抽搐振幅的浓度)值从53降至18mM,d-筒箭毒素分别降至0.7至0.3mM [3]。

[体内研究]

通过用单胺氧化酶抑制剂处理并通过儿茶酚-O-甲基转移酶抑制剂强化,可以在体内完全消除MPTP的毒性作用[1]。别嘌呤醇增强MPTP(35 mg/kg)诱导的DOPAC + HVA/DA比率下降和大鼠纹状体AA氧化增加[2]。在动物模型中,LPS或MPTP损伤的大多数反应性星形胶质细胞中Gas1的表达显着升高[4]。

[动物实验]

为了制备LPS大鼠模型和MPTP小鼠模型，进行动物的处理。简而言之，成年大鼠在以下坐标（AP-4.2 mm，L 1.5 mm和V 7.8 mm）处单侧注射LPS（0.5μL10μg/μL稀释于0.9％盐水中）至内侧前脑束（MFB），并用相同体积的0.9％生理盐水进入对侧。给成年小鼠腹膜内注射25mg / kg的MPTP连续5天，并注射相同体积的盐水作为对照。在LPS或MPTP注射后第1,2,3或4周处死所有动物。收集脑样品用于随后的免疫组织化学和蛋白质印迹实验。

[参考文献]

[1]. Langston J W, Irwin I. MPTP Neurotoxicity: An Overview and Characterization of Phases of Toxicity. II. Selective Accumulation of MPP in the Substantia Nigra: A Key to Neurotoxicity (Question). Life Sci., 1985, 36, No. 3, 201-12.

[2]. Desole M S, et al. Further investigation of allopurinol effects on MPTP-induced oxidative stress in the striatum and brain stem of the rat. Source:Pharmacol.Biochem.Behav., 1996, 54, No. 2, 377-83.

[3]. Hsu K S, et al. Potentiation of MPTP by 4-Phenylpyridine on the Neuromuscular Blockade in Mouse Phrenic Nerve-Diaphragm. Neuropharmacology, 1993, 32, No. 9, 877-83.

[4]. Sun XL, et al. Gas1 up-regulation is inducible and contributes to cell apoptosis in reactive astrocytes in the substantia nigra of LPS and MPTP models. J Neuroinflammation. 2016 Jul 8;13(1):180.

[相关活性小分子]

1-甲基-4-苯基-1,2,3,6-四氢吡啶盐酸盐物理化学性质

[ 沸点 ]:
258.6ºC at 760mmHg

[ 熔点 ]:
254 - 257 °C

[ 分子式 ]:
C₁₂H₁₆ClN

[ 分子量 ]:
209.715

[ 闪点 ]:
105.8ºC

[ 精确质量 ]:
209.097122

[ PSA ]:
3.24000

[ LogP ]:
3.14540

[ 外观性状 ]:
白色到灰白色粉末

[ 蒸汽压 ]:
0.0136mmHg at 25°C

[ 储存条件 ]:
室温，干燥，密封

1-甲基-4-苯基-1,2,3,6-四氢吡啶盐酸盐MSDS

详细MSDS(安全技术说明书)

1-甲基-4-苯基-1,2,3,6-四氢吡啶盐酸盐毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UT8358950

CHEMICAL NAME :: Pyridine, 1,2,3,6-tetrahydro-1-methyl-4-phenyl-, hydrochloride

CAS REGISTRY NUMBER :: 23007-85-4

LAST UPDATED :: 199603

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C12-H15-N.Cl-H

MOLECULAR WEIGHT :: 209.74

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 72 mg/kg

TOXIC EFFECTS :: Behavioral - tremor Behavioral - convulsions or effect on seizure threshold Behavioral - changes in motor activity (specific assay)

REFERENCE :: BEXBAN Bulletin of Experimental Biology and Medicine (English Translation). Translation of BEBMAE. (Plenum Pub. Corp., 233 Spring St., New York, NY 10013) V.41- 1956- Volume(issue)/page/year: 105,470,1988

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 53800 ug/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - changes in motor activity (specific assay) Gastrointestinal - changes in structure or function of salivary glands

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 247,531,1988 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 150 mg/kg/5D-I

TOXIC EFFECTS :: Brain and Coverings - other degenerative changes Nutritional and Gross Metabolic - changes in metals, not otherwise specified Biochemical - Neurotransmitters or modulators (putative) - dopamine in striatum

REFERENCE :: PHTOEH Pharmacology and Toxicology (Copenhagen). (Munksgaard International Pub., POB 2148, DK-1016 Copenhagen K, Denmark) V.60- 1987- Volume(issue)/page/year: 76,348,1995 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 40 mg/kg

SEX/DURATION :: female 15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - extra-embryonic structures (e.g., placenta, umbilical cord) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

REFERENCE :: TXCYAC Toxicology. (Elsevier Scientific Pub. Ireland, Ltd., POB 85, Limerick, Ireland) V.1- 1973- Volume(issue)/page/year: 67,63,1991

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 25 mg/kg

SEX/DURATION :: female 17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - maternal-fetal exchange

REFERENCE :: JONRA9 Journal of Neurochemistry. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) V.1- 1956- Volume(issue)/page/year: 55,1427,1990

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 35 mg/kg

SEX/DURATION :: female 12-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - biochemical and metabolic Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - other hydrolases

REFERENCE :: LIFSAK Life Sciences. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.1-8, 1962-69; V.14- 1974- Volume(issue)/page/year: 48,217,1991

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1-甲基-4-苯基-1,2,3,6-四氢吡啶盐酸盐安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301 + H311 + H331-H315-H319-H335

[ 警示性声明 ]:
P261-P280-P301 + P310-P305 + P351 + P338-P311

[ 危害码 (欧洲) ]:
T: Toxic;

[ 风险声明 (欧洲) ]:
R25;R39/23/24/25

[ 危险品运输编码 ]:
UN 2811

[ RTECS号 ]:
UT8358950

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2933399090

1-甲基-4-苯基-1,2,3,6-四氢吡啶盐酸盐海关

[ 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%

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