JHU 37160
Chemical Name: 8-Chloro-11-(4-ethylpiperazin-1-yl)-4-fluoro-5H-dibenzo[b,e][1,4]diazepine
Purity: ≥98%
Biological Activity
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 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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High-potency ligands for DREADD imaging and activation in rodents and monkeys.
Bonaventura et al.
Nat.Commun., 2019;10:4627
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