JHU37152 is a high affinity, highly potent, BBB penetrant activator (agonist) of hM3Dq and hM4Di DREADDs with Ki 1.8 nM and 8.7 nM for hM3Dq and hM4Di in vitro. JHU37152 selectively displaces [3H]clozapine from DREADDs in vivo, but not from other clozapine binding sites. JHU37152 inhibits locomotor activity in mice expressing hM3Dq and hM4Di in D1-expressing neurons. Designer receptors exclusively activated by designer drugs (DREADD) technology is a powerful chemogenetic approach used for neuromodulation in uninstrumented research animals.
Physicochemical Properties
M.Wt
358.85
Formula
C19H20ClFN4
Appearance
Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Month
Shipping
Solubility
Chemical Name/SMILES
References
1. Jordi Bonaventura, et al. Nat Commun. 2019 Oct 11;10(1):4627.
