洛贝林

• 常用名: 洛贝林
• 英文名: (-)-Lobeline
• CAS号: 90-69-7
• 分子量: 337.455
• 密度: 1.1±0.1 g/cm3
• 沸点: 485.6±15.0 °C at 760 mmHg
• 分子式: C₂₂H₂₇NO₂
• 熔点: 130-131°
• 闪点: 247.5±20.4 °C

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]。

洛贝林名称

• 中文名: 洛贝林
• 英文名: (-)-lobeline

洛贝林生物活性

• 描述: 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]。
• 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

Date Updated: 13/FEB/2006
Version 1.2
Regulation (EC) No 1907/2006
________________________________________________________________________
1 - Product and Company Information
________________________________________________________________________

Product NameL-LOBELINE FREE BASE
Product NumberL7149
Company
Century Ba-Shi Building 22A-B,
200020 Shanghai
Technical Phone #86-21-61415566
Fax 86-21-61415567
E-mail Address
________________________________________________________________________
2 - Hazards Identification
________________________________________________________________________
SPECIAL INDICATION OF HAZARDS TO HUMANS AND THE ENVIRONMENT
Toxic by inhalation, in contact with skin and if swallowed.
________________________________________________________________________
3 - Composition/Information on Ingredients
________________________________________________________________________
Product NameCAS #EC noAnnex I
Index Number
L-LOBELINE FREE BASE90-69-7202-012-3 None
FormulaC22H27NO2
Molecular Weight 337,5000 AMU
Synonyms8,10-Diphenyllobelionol *
2-(6-(beta-Hydroxy-phenethyl)-1-methyl-2-piperidy
l)acetophenone *
2-(6-(2-Hydroxy-2-phenylethyl)-1-methyl-2-piperid
inyl)-1-phenylethanone * Inflatine * Lobelin *
(-)-Lobeline * alpha-Lobeline * Lobnico
________________________________________________________________________
4 - First Aid Measures
________________________________________________________________________
AFTER INHALATION
If inhaled, remove to fresh air. If breathing becomes difficult,
call a physician.
AFTER SKIN CONTACT
In case of skin contact, flush with copious amounts of water for
at least 15 minutes. Remove contaminated clothing and shoes.
Call a physician.
AFTER EYE CONTACT
In case of contact with eyes, flush with copious amounts of
water for at least 15 minutes. Assure adequate flushing by
separating the eyelids with fingers. Call a physician.
AFTER INGESTION
If swallowed, wash out mouth with water provided person is
conscious. Call a physician.
________________________________________________________________________
5 - Fire Fighting Measures
________________________________________________________________________
EXTINGUISHING MEDIA
Suitable: Carbon dioxide, dry chemical powder, or appropriate
foam.
SPECIAL PROTECTIVE EQUIPMENT FOR FIREFIGHTERS
Wear self-contained breathing apparatus and protective clothing
to prevent contact with skin and eyes.
________________________________________________________________________
6 - Accidental Release Measures
________________________________________________________________________
PROCEDURE(S) OF PERSONAL PRECAUTION(S)
Wear respirator, chemical safety goggles, rubber boots, and
heavy rubber gloves.
METHODS FOR CLEANING UP
Sweep up, place in a bag and hold for waste disposal. Avoid
raising dust. Ventilate area and wash spill site after material
pickup is complete.
________________________________________________________________________
7 - Handling and Storage
________________________________________________________________________
________________________________________________________________________
8 - Exposure Controls / Personal Protection
________________________________________________________________________
ENGINEERING CONTROLS
Mechanical exhaust.
PERSONAL PROTECTIVE EQUIPMENT
Respiratory Protection: Use respirators and components tested and
approved under appropriate government standards such as NIOSH (US)
or CEN (EU). Where risk assessment shows air-purifying respirators
are appropriate use a full-face particle respirator type N99 (US)
or type P2 (EN 143) respirator cartridges as a backup to
engineering controls. If the respirator is the sole means of
protection, use a full-face supplied air respirator.
Hand Protection: Compatible chemical-resistant gloves.
Eye Protection: Chemical safety goggles.
________________________________________________________________________
9 - Physical and Chemical Properties
________________________________________________________________________
AppearancePhysical State: Solid
PropertyValueAt Temperature or Pressure
pHN/A
BP/BP RangeN/A
MP/MP RangeN/A
Flash PointN/A
FlammabilityN/A
Autoignition TempN/A
Oxidizing PropertiesN/A
Explosive PropertiesN/A
Explosion LimitsN/A
Vapor PressureN/A
Partition CoefficientN/A
ViscosityN/A
Vapor DensityN/A
Saturated Vapor Conc. N/A
Evaporation RateN/A
Bulk DensityN/A
Decomposition Temp.N/A
Solvent ContentN/A
Water ContentN/A
Surface TensionN/A
ConductivityN/A
Miscellaneous DataN/A
SolubilityN/A
________________________________________________________________________
10 - Stability and Reactivity
________________________________________________________________________
STABILITY
Stable: Stable.
HAZARDOUS DECOMPOSITION PRODUCTS
Hazardous Decomposition Products: Carbon monoxide, Carbon dioxide,
Nitrogen oxides.
HAZARDOUS POLYMERIZATION
Hazardous Polymerization: Will not occur
________________________________________________________________________
11 - Toxicological Information
________________________________________________________________________
RTECS NUMBER: OJ8480000
ACUTE TOXICITY
LD50
Intraperitoneal
Mouse
43500 UG/KG
LD50
Intravenous
Mouse
6300 UG/KG
LD50
Subcutaneous
Rabbit
35 MG/KG
SIGNS AND SYMPTOMS OF EXPOSURE
Stomach pains, vomiting, diarrhea. Exposure can cause:
ROUTE OF EXPOSURE
Multiple Routes: Harmful if swallowed, inhaled, or absorbed
through skin. May cause irritation.
TARGET ORGAN INFORMATION
Central nervous system. Peripheral nervous system.
________________________________________________________________________
12 - Ecological Information
________________________________________________________________________
No data available.
________________________________________________________________________
13 - Disposal Considerations
________________________________________________________________________
SUBSTANCE DISPOSAL
Dissolve or mix the material with a combustible solvent and burn
in a chemical incinerator equipped with an afterburner and
scrubber. Observe all federal, state, and local environmental
regulations.
________________________________________________________________________
14 - Transport Information
________________________________________________________________________
RID/ADR
UN#: 1544
Class: 6.1
PG: III
Proper Shipping Name: Alkaloids, solid, n.o.s.
IMDG
UN#: 1544
Class: 6.1
PG: III
Proper Shipping Name: Alkaloids, solid, n.o.s.
Marine Pollutant: No
Severe Marine Pollutant: No
Technical Name: Required
IATA
UN#: 1544
Class: 6.1
PG: III
Proper Shipping Name: Alkaloids, solid, n.o.s.
Inhalation Packing Group I: No
Technical Name: Required
________________________________________________________________________
15 - Regulatory Information
________________________________________________________________________
CLASSIFICATION AND LABELING ACCORDING TO EU DIRECTIVES
INDICATION OF DANGER: T
Toxic.
R-PHRASES: 23/24/25
Toxic by inhalation, in contact with skin and if swallowed.
S-PHRASES: 36/37/39-45
Wear suitable protective clothing, gloves, and eye/face
protection. In case of accident or if you feel unwell, seek
medical advice immediately (show the label where possible).
COUNTRY SPECIFIC INFORMATION
Germany
WGK: 3
Self-Classification
________________________________________________________________________
16 - Other Information
________________________________________________________________________
WARRANTY
The above information is believed to be correct but does not
purport to be all inclusive and shall be used only as a guide. The
information in this document is based on the present state of our
knowledge and is applicable to the product with regard to
appropriate safety precautions. It does not represent any
shall not be held liable for any damage resulting from handling or
from contact with the above product. See reverse side of invoice
or packing slip for additional terms and conditions of sale.
unlimitedpaper copies for internal use only.
DISCLAIMER
For R&D use only. Not for drug, household or other uses.

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模块 15 - 法规信息
N/A

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模块16 - 其他信息
N/A

洛贝林毒性和生态

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)

洛贝林英文别名

• [2R-[2a,6a(S*)]]-2-[6-(2-Hydroxy-2-phenylethyl)-1-methyl-2-piperidinyl]-1-phenylethanone
• 2-{(2R,6S)-6-[(2S)-2-Hydroxy-2-phenylethyl]-1-methylpiperidin-2-yl}-1-phenylethanone
• 2-{(2R,6S)-6-[(2S)-2-Hydroxy-2-phenylethyl]-1-methyl-2-piperidinyl}-1-phenylethanone
• Ethanone, 2-[(2R,6S)-6-[(2S)-2-hydroxy-2-phenylethyl]-1-methyl-2-piperidinyl]-1-phenyl-
• lobeline
• Lobron
• Bantron
• Inflatine
• 2-[(2R,6S)-6-[(2S)-2-hydroxy-2-phenylethyl]-1-methylpiperidin-2-yl]-1-phenylethanone
• Zoolobelin
• Lobelina