Description

• JHU 37160 is a high affinity and highly potent activator of hM3Dq and hM4Di DREADDs (Ki values are 1.9 nM and 3.6 nM for hM3Dq and hM4Di in vitro , respectively; EC50 values are 18.5 nM and 0.2 nM for hM3Dq and hM4Di in vitro , respectively)
• Displays approximately 25-fold higher affinity for hM4Di compared to DREADD agonist 21 (Cat
• No
• 5548)
• Selectively displaces [3H]clozapine from DREADDs in vivo , but not from other clozapine binding sites
• Inhibits locomotor activity in mice expressing hM3Dq and hM4Di in D1-expressing neurons, and increases hM3Dq-stimulated locomotion in rats expressing hM3Dq in TH-expressing neurons
• Brain penetrant in mice, rats and non-human primates.