Compound21(DREADDagonist21)isananalogofclozapineN-oxide(CNO). Watersolublehydrochloridesaltalsoavailable.
Compound21(DREADDagonist21)isahighlypotentagonistattheexcitatoryhM3DqDREADD(EC50 =1.7nM)whichshowshighselectivityforactivatinghM3DqcomparedtothenativehM3 muscarinicreceptorandotherGPCRs.
Compound21hasminimaloff-targetactivity.ThereareindicationsthatCompound21cannotbemetabolizedvianormalroutestoclozapine(oranyrelatedcompound)and thatCompound21hasequivalentpotencyinvivowhencomparedwith clozapineN-oxide.
UnpublisheddataindicatesthatCompound21(DREADDagonist21)activatestheinhibitoryhM4DDREADD.
Unpublisheddataalsosuggestsusingadoseof3mg/kginratmodels.
Compound21therefore representsanalternativetoCNO.
Purity>98%
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Properties
- Chemicalname
11-(1-Piperazinyl)-5H-dibenzo[b,e][1,4]diazepine
- MolecularWeight
278.35
- Chemicalstructure
- MolecularFormula
C17H18N4
- CASNumber
56296-18-5
- PubChemidentifier
11818276
- SMILES
C1CN(CCN1)C2=NC3=CC=CC=C3NC4=CC=CC=C42
- Source
Synthetic
- InChi
InChI=1S/C17H18N4/c1-2-6-14-13(5-1)17(21-11-9-18-10-12-21)20-16-8-4-3-7-15(16)19-14/h1-8,18-19H,9-12H2
- InChiKey
JCBYXNSOLUVGTF-UHFFFAOYSA-N
- Appearance
Yellowsolid
StoringandUsingYourProduct
ReferencesforCompound21(DREADDagonist21)
Thefirststructure-activityrelationshipstudiesfordesignerreceptorsexclusivelyactivatedbydesignerdrugs.
Chenetal(2015)ACSChemNeurosci6(3):476-84PubMedID:25587888
OptogeneticapproachesfordissectingneuromodulationandGPCRsignalinginneuralcircuits.
SpanglerandBruchas(2017)CurrOpinPharmacol32:56-70.PubMedID:27875804
ClozapineN-OxideAdministrationProducesBehavioralEffectsinLong-EvansRats:ImplicationsforDesigningDREADDExperiments.
MacLarenetal(2016)eNeuro3(5):0219-16PubMedID:27822508
Newnon-CNOactuatorsforDREADDs
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