洛贝林
洛贝林
常用名:洛贝林
CAS号:90-69-7
英文名:(-)-Lobeline
中文别名:N/A
洛贝林名称
中文名:洛贝林
英文名:(-)-lobeline
英文别名:更多
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1μMd-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(0.3-3.0mg/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(3mg/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(200-250g)[3]剂量:0.3mg/kg、1.0mg/kg和3.0mg/kg用于急性给药;慢性给药3mg/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(0.05mg/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].TengL,etal.Lobelineandnicotineevoke[3H]overflowfromratstriatalslicespreloadedwith[3H]dopamine:differentialinhibitionofsynaptosomalandvesicular[3H]dopamineuptake.JPharmacolExpTher.1997Mar;280(3):1432-44.
[2].MillerDK,etal.Lobelineinhibitstheneurochemicalandbehavioraleffectsofamphetamine.JPharmacolExpTher.2001Mar;296(3):1023-34.
[3].HarrodSB,etal.Lobelineattenuatesd-methamphetamineself-administrationinrats.JPharmacolExpTher.2001Jul;298(1):172-9.
洛贝林物理化学性质
密度:1.1±0.1g/cm3
沸点:485.6±15.0°Cat760mmHg
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±1.3mmHgat25°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
:DateUpdated:13/FEB/2006
Version1.2
Regulation(EC)No1907/2006
________________________________________________________________________
1-ProductandCompanyInformation
________________________________________________________________________
ProductNameL-LOBELINEFREEBASE
ProductNumberL7149
Company
CenturyBa-ShiBuilding22A-B,
200020Shanghai
TechnicalPhone#86-21-61415566
Fax86-21-61415567
E-mailAddress
________________________________________________________________________
2-HazardsIdentification
________________________________________________________________________
SPECIALINDICATIONOFHAZARDSTOHUMANSANDTHEENVIRONMENT
Toxicbyinhalation,incontactwithskinandifswallowed.
________________________________________________________________________
3-Composition/InformationonIngredients
________________________________________________________________________
ProductNameCAS#ECnoAnnexI
IndexNumber
L-LOBELINEFREEBASE90-69-7202-012-3None
FormulaC22H27NO2
MolecularWeight337,5000AMU
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-FirstAidMeasures
________________________________________________________________________
AFTERINHALATION
Ifinhaled,removetofreshair.Ifbreathingbecomesdifficult,
callaphysician.
AFTERSKINCONTACT
Incaseofskincontact,flushwithcopiousamountsofwaterfor
atleast15minutes.Removecontaminatedclothingandshoes.
Callaphysician.
AFTEREYECONTACT
Incaseofcontactwitheyes,flushwithcopiousamountsof
waterforatleast15minutes.Assureadequateflushingby
separatingtheeyelidswithfingers.Callaphysician.
AFTERINGESTION
Ifswallowed,washoutmouthwithwaterprovidedpersonis
conscious.Callaphysician.
________________________________________________________________________
5-FireFightingMeasures
________________________________________________________________________
EXTINGUISHINGMEDIA
Suitable:Carbondioxide,drychemicalpowder,orappropriate
foam.
SPECIALPROTECTIVEEQUIPMENTFORFIREFIGHTERS
Wearself-containedbreathingapparatusandprotectiveclothing
topreventcontactwithskinandeyes.
________________________________________________________________________
6-AccidentalReleaseMeasures
________________________________________________________________________
PROCEDURE(S)OFPERSONALPRECAUTION(S)
Wearrespirator,chemicalsafetygoggles,rubberboots,and
heavyrubbergloves.
METHODSFORCLEANINGUP
Sweepup,placeinabagandholdforwastedisposal.Avoid
raisingdust.Ventilateareaandwashspillsiteaftermaterial
pickupiscomplete.
________________________________________________________________________
7-HandlingandStorage
________________________________________________________________________
________________________________________________________________________
8-ExposureControls/PersonalProtection
________________________________________________________________________
ENGINEERINGCONTROLS
Mechanicalexhaust.
PERSONALPROTECTIVEEQUIPMENT
RespiratoryProtection:Userespiratorsandcomponentstestedand
approvedunderappropriategovernmentstandardssuchasNIOSH(US)
orCEN(EU).Whereriskassessmentshowsair-purifyingrespirators
areappropriateuseafull-faceparticlerespiratortypeN99(US)
ortypeP2(EN143)respiratorcartridgesasabackupto
engineeringcontrols.Iftherespiratoristhesolemeansof
protection,useafull-facesuppliedairrespirator.
HandProtection:Compatiblechemical-resistantgloves.
EyeProtection:Chemicalsafetygoggles.
________________________________________________________________________
9-PhysicalandChemicalProperties
________________________________________________________________________
AppearancePhysicalState:Solid
PropertyValueAtTemperatureorPressure
pHN/A
BP/BPRangeN/A
MP/MPRangeN/A
FlashPointN/A
FlammabilityN/A
AutoignitionTempN/A
OxidizingPropertiesN/A
ExplosivePropertiesN/A
ExplosionLimitsN/A
VaporPressureN/A
PartitionCoefficientN/A
ViscosityN/A
VaporDensityN/A
SaturatedVaporConc.N/A
EvaporationRateN/A
BulkDensityN/A
DecompositionTemp.N/A
SolventContentN/A
WaterContentN/A
SurfaceTensionN/A
ConductivityN/A
MiscellaneousDataN/A
SolubilityN/A
________________________________________________________________________
10-StabilityandReactivity
________________________________________________________________________
STABILITY
Stable:Stable.
HAZARDOUSDECOMPOSITIONPRODUCTS
HazardousDecompositionProducts:Carbonmonoxide,Carbondioxide,
Nitrogenoxides.
HAZARDOUSPOLYMERIZATION
HazardousPolymerization:Willnotoccur
________________________________________________________________________
11-ToxicologicalInformation
________________________________________________________________________
RTECSNUMBER:OJ8480000
ACUTETOXICITY
LD50
Intraperitoneal
Mouse
43500UG/KG
LD50
Intravenous
Mouse
6300UG/KG
LD50
Subcutaneous
Rabbit
35MG/KG
SIGNSANDSYMPTOMSOFEXPOSURE
Stomachpains,vomiting,diarrhea.Exposurecancause:
ROUTEOFEXPOSURE
MultipleRoutes:Harmfulifswallowed,inhaled,orabsorbed
throughskin.Maycauseirritation.
TARGETORGANINFORMATION
Centralnervoussystem.Peripheralnervoussystem.
________________________________________________________________________
12-EcologicalInformation
________________________________________________________________________
Nodataavailable.
________________________________________________________________________
13-DisposalConsiderations
________________________________________________________________________
SUBSTANCEDISPOSAL
Dissolveormixthematerialwithacombustiblesolventandburn
inachemicalincineratorequippedwithanafterburnerand
scrubber.Observeallfederal,state,andlocalenvironmental
regulations.
________________________________________________________________________
14-TransportInformation
________________________________________________________________________
RID/ADR
UN#:1544
Class:6.1
PG:III
ProperShippingName:Alkaloids,solid,n.o.s.
IMDG
UN#:1544
Class:6.1
PG:III
ProperShippingName:Alkaloids,solid,n.o.s.
MarinePollutant:No
SevereMarinePollutant:No
TechnicalName:Required
IATA
UN#:1544
Class:6.1
PG:III
ProperShippingName:Alkaloids,solid,n.o.s.
InhalationPackingGroupI:No
TechnicalName:Required
________________________________________________________________________
15-RegulatoryInformation
________________________________________________________________________
CLASSIFICATIONANDLABELINGACCORDINGTOEUDIRECTIVES
INDICATIONOFDANGER:T
Toxic.
R-PHRASES:23/24/25
Toxicbyinhalation,incontactwithskinandifswallowed.
S-PHRASES:36/37/39-45
Wearsuitableprotectiveclothing,gloves,andeye/face
protection.Incaseofaccidentorifyoufeelunwell,seek
medicaladviceimmediately(showthelabelwherepossible).
COUNTRYSPECIFICINFORMATION
Germany
WGK:3
Self-Classification
________________________________________________________________________
16-OtherInformation
________________________________________________________________________
WARRANTY
Theaboveinformationisbelievedtobecorrectbutdoesnot
purporttobeallinclusiveandshallbeusedonlyasaguide.The
informationinthisdocumentisbasedonthepresentstateofour
knowledgeandisapplicabletotheproductwithregardto
appropriatesafetyprecautions.Itdoesnotrepresentany
shallnotbeheldliableforanydamageresultingfromhandlingor
fromcontactwiththeaboveproduct.Seereversesideofinvoice
orpackingslipforadditionaltermsandconditionsofsale.
unlimitedpapercopiesforinternaluseonly.
DISCLAIMER
ForR&Duseonly.Notfordrug,householdorotheruses.
模块15-法规信息
N/A
模块16-其他信息
N/A
洛贝林毒性和生态
:
洛贝林毒性英文版
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:UN1544
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
洛贝林重点介绍
【洛贝林】凯途网洛贝林CAS号:90-69-7,洛贝林MSDS及其说明、性质、英文名、生产厂家、作用/用途、分子量、密度、沸点、熔点、结构式等。CAS号查询洛贝林。
原料药根据它的来源分为化学合成药和天然化学药两大类。 化学合成药又可分为无机合成药和有机合成药。无机合成药为无机化合物(极个别为元素),如用于治疗胃及十二指肠溃疡的氢氧化铝、三硅酸镁等;有机合成药主要是由基本有机化工原料,经一系列有机化学反应而制得的药物(如阿司匹林、氯霉素、咖啡因等)
LuoBeiLin
洛貝林
公司简介
广州佳途科技股份有限公司是一家专注于高难度小分子药物化学合成-放大生产的国家高新技术企业,现有员工超过180人,技术人员占比72%。基于多年小分子药物合成经验及技术积累,公司构建了硝化/氢化/超低温特殊反应技术平台、新分子设计合成技术平台、微通道连续反应生产应用平台,为客户提供专业的化合物合成CRO/CDMO服务。
资质荣誉
国家高新技术企业、国家标准样品专家咨询委员会委员、中国科技创新先进单位、广东省守合同重信用企业、广州市专精特新中小企业。
核心技术
- 硝化反应技术:
1.硝化剂筛选:针对不同的反应底物活性选择合适的硝化剂;
2.硝化方法筛选:从安全和操作方面筛选与反应底物匹配的硝化方法;
3.硝化工艺优化:通过平行反应筛选最佳的反应温度、体积、滴加速度等,以获得最优工艺;
4.反应安全性评估:对需要工业化生产的反应进行安全性评估,确保安全生产;
5.流体化学反应装置:通过流体化学反应技术,筛选适合的工艺,提高反应的安全性。 - 氢化反应技术:
1.催化剂筛选:筛选适合反应底物的催化剂;
2.氢化工艺优化:针对性的优化工艺,以达到成本低,绿色环保的目的;
3.反应安全性评估:选择合适的反应温度和压力,达到安全生产的目的。 - 超低温反应技术:
1.反应类型:技术人员具有格式反应、锂化反应、低温环化反应等低温反应经验;
2.工艺优化:通过平行反应筛选最佳的反应温度、体积、滴加速度等,以获得最优工艺;
3.操作安全性评估:对反应各环节严格把控,确保安全;
4.反应装置:实验室配备50L超低温反应釜和液氨罐,可满足-100℃-200℃反应。
研发&生产
中间体合成实验室:
工艺放大实验室:
分析实验室: