JHU 37152

Biological Activity

JHU 37152 is a high affinity and highly potent activator of hM₃D_q and hM₄D_i DREADDs (K_i values are 1.8 nM and 8.7 nM for hM₃D_q and hM₄D_i in vitro, respectively; EC₅₀ values are 5 nM and 0.5 nM for hM₃D_q and hM₄D_i in vitro, respectively). Selectively displaces [³H]clozapine from DREADDs in vivo, but not from other clozapine binding sites. Inhibits locomotor activity in mice expressing hM₃D_q and hM₄D_i in D₁-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

1. High-potency ligands for DREADD imaging and activation in rodents and monkeys.
   Bonaventura et al.
   Nat.Commun., 2019;10:4627

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