洛贝林

洛贝林用途

洛贝林(α-洛贝林；L-洛贝林)是一种亲脂性生物碱,是一种烟碱受体激动剂。洛贝林抑制d-甲基苯丙胺自我给药,无多巴胺毒性。洛贝琳挽救了滥用d-苯丙胺导致的成瘾效应。洛贝林通过抑制DA摄取到突触小泡中并改变突触前DA储存来增加多巴胺(DA)释放[1][2][3]。

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洛贝林名称

[ CAS 号 ]:
90-69-7

[ 中文名 ]:
洛贝林

[ 英文名 ]:
(-)-Lobeline

[英文别名 ]:

lobeline
Lobron
Bantron
Inflatine
Zoolobelin
Lobelina

洛贝林生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 胆碱受体

信号通路 >> 神经信号通路 >> 胆碱受体

信号通路 >> 神经信号通路 >> 多巴胺转运蛋白

研究领域 >> 神经疾病

[体外研究]

洛贝林(0.1-100μM)诱导 [3H]天溢出呈非钙依赖性[1]。洛贝琳牌手表抑制 [3H]天被突触小体 (IC50=80μM)和囊泡 (IC50=0.88μM)摄取[1]。洛贝林(0.1-1μM；1小时)抑制 1μM d-甲基苯丙胺诱导的纹状体切片释放多巴胺[2]。

[体内研究]

洛贝林(0.3-3.0 mg/kg；皮下注射; 单剂量) 降低模型大鼠 d-去氧麻黄碱的自我给药能力[3]。洛贝林(3 mg/kg；皮下注射; 7.个周期,共 7.次) 以非竞争性的方式特别降低大鼠对 d-去氧麻黄碱的反应,并增加耐受性发展[3]。动物模型：Sprague-Dawley大鼠(200-250 g)[3]剂量：0.3 mg/kg、1.0 mg/kg和3.0 mg/kg用于急性给药；慢性给药3 mg/kg给药：皮下注射；测量前15分钟,或每15分钟进行7次；间隔2个干预维持日的d-甲基苯丙胺(0.05 mg/kg输注)自我给药结果：d-甲基苯甲酯自我给药减少。

[参考文献]

[1]. Teng L, et al. Lobeline and nicotine evoke [3H]overflow from rat striatal slices preloaded with [3H]dopamine: differential inhibition of synaptosomal and vesicular [3H]dopamine uptake. J Pharmacol Exp Ther. 1997 Mar;280(3):1432-44.

[2]. Miller DK, et al. Lobeline inhibits the neurochemical and behavioral effects of amphetamine. J Pharmacol Exp Ther. 2001 Mar;296(3):1023-34.

[3]. Harrod SB, et al. Lobeline attenuates d-methamphetamine self-administration in rats. J Pharmacol Exp Ther. 2001 Jul;298(1):172-9.

洛贝林物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
485.6±15.0 °C at 760 mmHg

[ 熔点 ]:
130-131°

[ 分子式 ]:
C₂₂H₂₇NO₂

[ 分子量 ]:
337.455

[ 闪点 ]:
247.5±20.4 °C

[ 精确质量 ]:
337.204193

[ PSA ]:
40.54000

[ LogP ]:
3.61

[ 蒸汽压 ]:
0.0±1.3 mmHg at 25°C

[ 折射率 ]:
1.563

[ 储存条件 ]:
库房低温通风干燥,与食品原料分开存放

洛贝林MSDS

详细MSDS(安全技术说明书)

洛贝林毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: OJ8480000

CHEMICAL NAME :: Lobeline

CAS REGISTRY NUMBER :: 90-69-7

BEILSTEIN REFERENCE NO. :: 0091533

LAST UPDATED :: 199612

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C22-H27-N-O2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 80 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold

REFERENCE :: AEPPAE Naunyn-Schmiedeberg's Archiv fuer Experimentelle Pathologie und Pharmakologie. (Berlin, Ger.) V.110-253, 1925-66. For publisher information, see NSAPCC. Volume(issue)/page/year: 132,63,1928

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 43500 ug/kg

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

REFERENCE :: STRAAA Strahlentherapie. (Urban & Schwarzenberg, Postfach 202440, D-8000 Munich 2, Fed. Rep. Ger.) V.1- 1912- Volume(issue)/page/year: 127,245,1965

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 100 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold

REFERENCE :: AEPPAE Naunyn-Schmiedeberg's Archiv fuer Experimentelle Pathologie und Pharmakologie. (Berlin, Ger.) V.110-253, 1925-66. For publisher information, see NSAPCC. Volume(issue)/page/year: 132,63,1928

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 6300 ug/kg

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

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 103,146,1955

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 35 mg/kg

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

REFERENCE :: FATOAO Farmakologiya i Toksikologiya (Moscow). For English translation, see PHTXA6 and RPTOAN. (V/O Mezhdunarodnaya Kniga, 113095 Moscow, USSR) V.2- 1939- Volume(issue)/page/year: 4(1),34,1941

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 10 mg/kg

TOXIC EFFECTS :: Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

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: 31,43,1927

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洛贝林安全信息

[ 危害码 (欧洲) ]:
T

[ 风险声明 (欧洲) ]:
23/24/25

[ 安全声明 (欧洲) ]:
36/37/39-45

[ 危险品运输编码 ]:
UN 1544

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

洛贝林

洛贝林用途

洛贝林名称

洛贝林生物活性

洛贝林物理化学性质

洛贝林MSDS

详细MSDS(安全技术说明书)

洛贝林毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

洛贝林安全信息

洛贝林合成路线

详细合成路线

洛贝林上下游产品

洛贝林上游产品

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