Compound21(DREADDagonist21)hydrochlorideisawatersolubleanalogofclozapineN-oxide(CNO).Freebasealsoavailable.
Compound21(DREADDagonist21)isahighlypotentagonistattheexcitatoryhM3DqDREADD(EC50=1.7nM)whichshowshighselectivityforactivatinghM3DqcomparedtothenativehM3muscarinicreceptorandotherGPCRs.
Compound21hasminimaloff-targetactivity.ThereareindicationsthatCompound21cannotbemetabolizedvianormalroutestoclozapine(oranyrelatedcompound)and thatCompound21hasequivalentpotencyinvivowhencomparedwith clozapineN-oxide.
UnpublisheddataindicatesthatCompound21(DREADDagonist21)activatestheinhibitoryhM4DDREADD.
Unpublisheddataalsosuggestsusingadoseof3mg/kginratmodels.
Compound21therefore representsanalternativetoCNO.

