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  5. Tocris Bioscience™ Deschloroclozapine

Tocris Bioscience™ Deschloroclozapine
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Catalog No. p-7237103
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Catalog No. Quantity
71-931-0 10 mg
71-935-0 50 mg
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Catalog No. 71-931-0 Supplier Tocris Bioscience™ Supplier No. 7193/10
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Description

High affinity and highly potent activator of hM3Dq and hM4Di DREADDs; rapidly blood brain barrier penetrant

Deschloroclozapine 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.

Specifications

Chemical Name or Material 11-(4-Methyl-1-piperazinyl)-5 H-dibenzo[b,e][1,4 ]diazepine
CAS 7-7-1977
Quantity 10 mg
Target DREADD Activators
Molecular Formula C18H20N4
Purity 0.98
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