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骆驼蓬灵

骆驼蓬灵用途

Harmaline 是动物体内有效,可逆的单胺氧化酶 (monoamine oxidase) 抑制剂。 Harmaline是一种中枢神经系统兴奋剂,可用于诱发啮齿动物的震颤。

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骆驼蓬灵名称

[ CAS 号 ]:
304-21-2

[ 中文名 ]:
骆驼蓬灵

[ 英文名 ]:
Harmaline

[中文别名 ]:

[英文别名 ]:

3,4-Dihydroharmine
Armalin
7-Methoxy-1-methyl-3,4-dihydro-2H-β-carboline
Harmine,dihydro
Harmalol methyl ether
EINECS 206-152-6
MFCD00004955
3,4-Dihydro-7-methoxy-1-methyl-β-carboline
Dihydroharmine
Harmidine

骆驼蓬灵生物活性

[ 描述 ]:

Harmaline 是动物体内有效,可逆的单胺氧化酶 (monoamine oxidase) 抑制剂。 Harmaline是一种中枢神经系统兴奋剂,可用于诱发啮齿动物的震颤。

[ 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 ]

Target: Monoamine oxidase[1]

[体外研究]

Harmaline抑制单胺氧化酶,从而增加单胺类神经递质的水平(例如,在大鼠中为7-70μM/ kg)[1]。 Harmaline诱导的啮齿动物震颤是特发性震颤的模型。震颤活动取决于harmaline剂量。一线临床基本震颤治疗普萘洛尔,扑米酮和加巴喷丁和γ-羟基丁酸(GHB)显着减弱了骆驼因诱发的震颤。抗惊厥药丙戊酸和卡马西平以及情绪稳定剂锂抑制骆驼因诱发的震颤。 γ-氨基-丁酸(GABA)受体亚型A受体激动剂muscimol减弱了骆驼因诱导的震颤。 Harmaline(30 mg/kg)通过N-甲基-D-天冬氨酸(NMDA)受体(竞争性和非竞争性NMDA受体拮抗剂)和AMPA受体阻断诱导小鼠震颤,降低骆驼因诱导的震颤[2]。

[动物实验]

大鼠[1] 160-190g Wistar白化大鼠，禁食16小时，单独或在皮下注射75mg / kg 5-羟色氨酸之前1小时接受不同剂量的Harmaline（0-70μM/ kg），10 mg / kg Ro 4-1284或100mg / kg异丙嗪。将动物断头并用分光光度法测量脑中的5-羟色胺（在用心脏的5-羟色氨酸进行的实验中）[1]。小鼠[2]在测试之前将组装的小鼠带到实验室中至少1小时以适应环境。用媒介物或测试化合物预处理20分钟（扑米酮60分钟）后，给药物未处理的小鼠注射哈马林（30mg / kg）并置于Tremor监测室内10分钟的适应期。在适应期后，测量小鼠的震颤活动8分钟[2]。

[参考文献]

[1]. Gey, K.F, et al. Effect of α-alkylated tryptamine derivatives on 5-hydroxytryptamine metabolism in vivo. Brit.J.Pharmacol. 19, 161-167(1962).

[2]. Paterson NE, et al. Pharmacological characterization of harmaline-induced tremor activity in mice. Eur J Pharmacol. 2009 Aug 15;616(1-3):73-80.

[相关活性小分子]

骆驼蓬灵物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
426.4±45.0 °C at 760 mmHg

[ 熔点 ]:
232-234 °C(lit.)

[ 分子式 ]:
C₁₃H₁₄N₂O

[ 分子量 ]:
214.263

[ 闪点 ]:
211.7±28.7 °C

[ 精确质量 ]:
214.110611

[ PSA ]:
37.38000

[ LogP ]:
0.66

[ 蒸汽压 ]:
0.0±1.0 mmHg at 25°C

[ 折射率 ]:
1.647

[ 储存条件 ]:
库房低温,通风,干燥,与食品原料分开存放

骆驼蓬灵MSDS

详细MSDS(安全技术说明书)

骆驼蓬灵毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UU9800000

CHEMICAL NAME :: 3H-Pyrido(3,4-b)indole, 4,9-dihydro-7-methoxy-1-methyl-

CAS REGISTRY NUMBER :: 304-21-2

BEILSTEIN REFERENCE NO. :: 0207310

LAST UPDATED :: 199612

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C13-H14-N2-O

MOLECULAR WEIGHT :: 214.29

WISWESSER LINE NOTATION :: T B656 DM HM CHJ F1 KO1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 120 mg/kg

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

REFERENCE :: VHTODE Veterinary and Human Toxicology. (American College of Veterinary and Comparative Toxicology, Publication Office, Comparative Toxicology, Manhattan, KS 66506) V.19- 1977- Volume(issue)/page/year: 33,276,1991

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 120 mg/kg

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

REFERENCE :: PSCBAY Psychopharmacology Service Center, Bulletin. (Bethesda, MD) V.1-3, 1961-65. For publisher information, see PSYBB9. Volume(issue)/page/year: 2,17,1963

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 20 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - excitement Behavioral - ataxia

REFERENCE :: NEPHBW Neuropharmacology. (Pergamon Press Ltd., Headington Hill Hall, Oxford OX3 OBW, UK) V.9- 1970- Volume(issue)/page/year: 10,15,1971 *** REVIEWS *** TOXICOLOGY REVIEW PISDDJ Pacific Information Service on Street Drugs. (J.K. Brown, School of Pharmacy, Univ. of the Pacific, Stockton, CA 95211) V.1- 1972(?)- Volume(issue)/page/year: 5(3-6),-,1977 TOXICOLOGY REVIEW CTOXAO Clinical Toxicology. (New York, NY) V.1-18, 1968-81. For publisher information, see JTCTDW. Volume(issue)/page/year: 12,1,1978

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骆驼蓬灵安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
R25

[ 安全声明 (欧洲) ]:
S22-S24/25

[ 危险品运输编码 ]:
1544

[ WGK德国 ]:
3

[ RTECS号 ]:
UU9800000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2933990090

骆驼蓬灵合成路线

详细合成路线

骆驼蓬灵上下游产品

骆驼蓬灵上游产品

骆驼蓬灵下游产品

骆驼蓬灵海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 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 ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

骆驼蓬灵文献

High-throughput screening for new psychoactive substances (NPS) in whole blood by DLLME extraction and UHPLC-MS/MS analysis.

J. Chromatogr. B. Analyt. Technol. Biomed. Life Sci. 1000 , 57-68, (2015)

The increasing number of new psychoactive substances (NPS) present in the illicit market render their identification in biological fluids/tissues of great concern for clinical and forensic toxicology....

Fast determination of harmala alkaloids in edible algae by capillary electrophoresis mass spectrometry.

Anal. Bioanal. Chem 407(13) , 3637-45, (2015)

The use of algae as a foodstuff is rapidly expanding worldwide from the East Asian countries, where they are also used for medical care. Harmala alkaloids (HAlk) are a family of bioactive compounds fo...

Rapid and sensitive detection of the inhibitive activities of acetyl- and butyryl-cholinesterases inhibitors by UPLC-ESI-MS/MS.

J. Pharm. Biomed. Anal. 94 , 215-20, (2014)

Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) are legitimate therapeutic targets for Alzheimer's disease. The classical approach for screening potential AChE/BChE inhibitors was develop...

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