Varenicline-15N3-hydrochloride-CP-526555-sup-15-sup-N-sub-3-sub-Hydrochloride-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEVarenicline-15N3hydrochlorideCat.No.:HY-10020SCASNo.:1244134-80-2Synonyms:CP526555-15N3Hydrochloride分⼦式:C₁₃H₁₄Cl₁₅N₃分⼦量:250.7作⽤靶点:nAChR;Isotope-LabeledCompounds作⽤通路:MembraneTransporter/IonChannel;NeuronalSignaling;Others储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Varenicline-15N3Hydrochloride(CP526555-15N3Hydrochloride)15N标记的VareniclineHydrochloride(HY-10020)。Varenicline(CP526555)具有⼝服活性的尼古丁依赖主介质α4β2烟碱型⼄酰胆碱受体(α4β2nAChR)的部分激动剂(IC50=250nM)。Varenicline也α6β2nAChR的部分激动剂和α6β2nAChR的完全激动剂。Varenicline可阻断尼古丁对nAChR的直接激动作⽤，同时以更温和的程度刺激nAChR，被⼴泛⽤作戒烟的辅助⼿段[1][2][3][4][5]。REFERENCES[1].KoegelenbergCF,etal.Efficacyofvareniclinecombinedwithnicotinereplacementtherapyvsvareniclinealoneforsmokingcessation:arandomizedclinicaltrial.JAMA.2014Jul;312(2):155-61.[2].MagnusCJ,etal.Ultrapotentchemogeneticsforresearchandpotentialclinicalapplications.Science.2019;364(6436):eaav5282.[3].KogaM,etal.Vareniclinepromotesendothelialcellmigrationbyloweringvascularendothelial-cadherinlevelsviatheactivatedα7nicotinicacetylcholinereceptor-mitogenactivatedproteinkinaseaxis.Toxicology.2017;390:1-9.[4].RenJ,etal.CounteringOpioid-inducedRespiratoryDepressioninMaleRatswithNicotinicAcetylcholineReceptorPartialAgonistsVareniclineandABT594.Anesthesiology.2020May;132(5):1197-1211.[5].MelloNK,etal.Effectsofchronicvareniclinetreatmentonnicotine,cocaine,andconcurrentnicotine+cocaineself-administration.Neuropsychopharmacology.2014Apr;39(5):1222-31.[6].RollemaH,etal.Vareniclinehasantidepressant-likeactivityintheforcedswimtestandaugmentssertraline'seffect.EurJPharmacol.2009Mar1;605(1-3):114-6.McePdfHeight1/1MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400