JHU 37152

JHU37152 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.8 nM and 8.7 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 5 nM and 0.5 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively.,hM4Di [1](Cell-free assay)hM3Dq [1](Cell-free assay)hM3Dq [1](Cell-free assay)hM4Di [1](Cell-free assay)0.5 nM(EC50)1.8 nM(Ki)5 nM(EC50)8.7 nM(Ki),JHU37152 is a potent DREADD agonist with high potency and efficacy in fluorescent and BRET-based assays in HEK-293 cells, whereas no responses are observed in untransfected HEK-293 cells.[1],JHU37152 exhibits high in vivo DREADD potency. JHU37152 exhibits selective [3H]clozapine displacement from DREADDs in brain tissue from WT and D1-DREADD mice.[1]