Chemical Name: 8-Chloro-11-(4-ethylpiperazin-1-yl)-4-fluoro-5H-dibenzo[b,e][1,4]diazepine
Biological ActivityJHU 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 0.2 nM and 18.5 nM for hM4Di and hM3Dq 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.
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High-potency ligands for DREADD imaging and activation in rodents and monkeys.
Bonaventura et al.
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