Deschloroclozapine

Biological Activity

Deschloroclozapine is a high affinity and highly potent activator of muscarinic DREADDs (K_i values are 6.3 nM for hM₃D_q and 4.2 nM for hM₄D_i, in vitro; EC₅₀ values are 0.13 nM for hM₃D_q and 0.081 nM for hM₄D_i, in vitro). Derivative of clozapine (Cat. No. 0444). Exhibits 100-fold greater affinity for hM₃D_q and hM₄D_i compared to clozapine N-oxide (CNO; Cat. No. 4936), and 50-fold greater affinity compared to DREADD agonist 21 (Cat. No. 5548). Displays low 'off-target' receptor binding (K_i >100 nM at majority of GPCRs, ion channels and transporters tested). Displays rapid (approx. 10 minutes after i.p injection) binding and activation of hM₃D_q and hM₄D_i in mice and non-human primates. Induces spatial memory deficits in non-human primates expressing hM₄D_i in the prefrontal cortex.

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. Deschloroclozapine, a potent and selective chemogenetic actuator enables rapid neuronal and behavioral modulations in mice and monkeys
   Nagai et al.
   Nat.Neurosci., 2020;23:1157

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