Tocris Bioscience™ Deschloroclozapine
High affinity and highly potent activator of hM3Dq and hM4Di DREADDs; rapidly blood brain barrier penetrant
Manufacturer: Tocris Bioscience™ 7193/10
DescriptionDeschloroclozapine is a high affinity and highly potent activator of muscarinic DREADDs (Ki values are 6.3 nM for hM3Dq and 4.2 nM for hM4Di, in vitro; EC50 values are 0.13 nM for hM3Dq and 0.081 nM for hM4Di, in vitro). Derivative of clozapine (Cat. No. 0444). Exhibits 100-fold greater affinity for hM3Dq and hM4Di 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 (Ki >100 nM at majority of GPCRs, ion channels and transporters tested). Displays rapid (approx. 10 minutes after i.p injection) binding and activation of hM3Dq and hM4Di in mice and non-human primates. Induces spatial memory deficits in non-human primates expressing hM4Di in the prefrontal cortex.
|11-(4-Methyl-1-piperazinyl)-5 H-dibenzo[b,e][1,4 ]diazepine|
Safety and Handling
Recommended Storage : Store at RT