Deschloroclozapine is a high affinity and highly potent activator of muscarinic DREADDs. It is a derivative of clozapine, and exhibits 100-fold greater affinity for hM3Dq and hM4Di compared to clozapine N-oxide, and 50-fold greater affinity compared to DREADD agonist 21. Deschloroclozapine displays low 'off-target' receptor binding and rapid binding and activation of hM3Dq and hM4Di in mice and non-human primates. It also induces spatial memory deficits in non-human primates expressing hM4Di in the prefrontal cortex.
CAS Number: 1977-07-7
Molecular Weight: 292.38
11-(4-Methyl-1-piperazinyl)-5H-dibenzo(b, e)(1, 4)diazepine
Dopamine serotonin antagonist-1
11-(4-Methylpiperazin-1-yl)-5H-dibenzo[b, e][1, 4]diazepine
11-(4-Methyl-piperazin-1-yl)-5H-dibenzo[b, e][1, 4]diazepine
5H-DIBENZO(b, e)(1, 4)DIAZEPINE, 11-(4-METHYL-1-PIPERAZINYL)-
11-(4-Methyl-1-piperazinyl)-5H-dibenzo[b, e][1, 4]diazepine
5-25-11-00363 (Beilstein Handbook Reference)
5H-Dibenzo[b, e][1, 4]diazepine, 11-(4-methyl-1-piperazinyl)-
Chemical Name: 11-(4-methylpiperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepine
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
Deschloroclozapine has greater potencies for DREADDs than previous agonists in vitro. Deschloroclozapine is a potent agonist for hM3Dq with an EC50=0.13 nM. Deschloroclozapine is also a potent agonist for hM4Di with an EC50=0.081 nM. Deschloroclozapine is a potent and selective agonist for hM3Dq and hM4Di, it does not display significant agonistic activity for any of the 318 tests wild-type GPCRs at <10 nM.
Deschloroclozapine (100 μg/kg; i.v.) exhibits good brain concentration profiles and biostability. Pharmacokinetic studies confirmed that Deschloroclozapine is rapidly accumulated in mouse brains and monkey CSF, while its metabolites are negligible. Deschloroclozapine (1 μg/kg; i.p.) selectively and rapidly enhances neuronal activity via hM3Dq-DREADD in vivo, Deschloroclozapine can also be utilized for in vivo neuronal silencing by activating hM4Di, an inhibitory DREADD. Deschloroclozapine (1-100 μg/kg; i.v.) selectively induces hM3Dq-mediated metabolic activity. Deschloroclozapine (100 μg/kg; i.m.) selectively induces behavioral deficits in hM4Di-expressing monkeys.
- Upright NA, Baxter MG. Effect of chemogenetic actuator drugs on prefrontal cortex-dependent working memory in nonhuman primates. Neuropsychopharmacology. 2020 Oct;45(11):1793-1798. doi: 10.1038/s41386-020-0660-9. Epub 2020 Mar 19. PMID: 32193513.
- Maggs JL, Williams D, Pirmohamed M, Park BK. The metabolic formation of reactive intermediates from clozapine, a drug associated with agranulocytosis in man. J Pharmacol Exp Ther. 1995 Dec;275(3):1463-75. PMID: 8531117.
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