Deschloroclozapine (DCZ)
Product overview
| Name | Deschloroclozapine (DCZ) |
| Description | Potent, selective and metabolically stable hM3Dq and hM4Di muscarinic DREADD actuator. |
| Alternative names | DCZ |
| Purity | >98% |
Images
Biological Data
| Biological description | Overview Deschloroclozapine (DCZ) is reported to be a potent, selective and highly brain-penetrable muscarinic hM3Dq and hM4Di DREADD actuator with minimal off-target actions (Ki = 6.3 and 4.2 nM at hM3Dq and hM4Di respectively) and (EC50 values are 0.13 and 0.081 nM at hM3Dq and hM4Di respectively in a BRET-based assay. It represents a potent, selective, metabolically stable and fast acting DREADD agonist with utility in both mice and non-human primates for a variety of applications. It shows 100-fold improved affinity and greater agonist potency for hM3Dq and hM4Di compared to Clozapine n-Oxide (CNO) or DREADD agonist 21 (C21) with reduced off-target binding compared with clozapine in vitro.It has lower affinity at D1, D2 and 5-HT2A and 5-HT2C receptors compared with clozapine. PET studies demonstrate the compound is rapidly brain penetrable, is apparently selective and doses for DREADD occupancy are 20-fold and 60-fold lower than CNO or DREADD agonist 21 (C21) respectively. Uses and applications Systemic delivery of low doses of DCZ (1 or 3 µg/kg) were shown to enhance neuronal activity via hM3Dq in mice and monkeys within minutes. Intramuscular doses of 100 µg/kg reversibly induced spatial working memory deficits in hM4Di expressing monkeys. Deschloroclozapine dihydrochloride (water soluble) also available. |
Solubility & Handling
| Storage instructions | Room temperature |
| Solubility overview | Soluble in DMSO (100 mM), and in ethanol (50 mM with warming) |
| Important | This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use |
Chemical Data
| Chemical name | 6-(4-methylpiperazin-1-yl)-11H-benzo[b][1,4]benzodiazepine |
| Molecular Weight | 292.38 |
| Chemical structure | ![Deschloroclozapine [1977-07-7] Chemical Structure](https://hellobio.com/media/catalog/product//h/b/hb8555_1.png "Deschloroclozapine [1977-07-7]") |
| Molecular Formula | C18H20N4 |
| CAS Number | 1977-07-7 |
| PubChem identifier | 16103 |
| SMILES | CN1CCN(CC1)C2=NC3=CC=CC=C3NC4=CC=CC=C42 |
| Source | Synthetic |
| InChi | InChI=1S/C18H20N4/c1-21-10-12-22(13-11-21)18-14-6-2-3-7-15(14)19-16-8-4-5-9-17(16)20-18/h2-9,19H,10-13H2,1H3 |
| InChiKey | VQHITFFJBFOMBG-UHFFFAOYSA-N |
| Appearance | Yellow solid |
References for Deschloroclozapine (DCZ)
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Deschloroclozapine, a potent and selective chemogenetic actuator enables rapid neuronal and behavioral modulations in mice and monkeys
Nagai et al (2020) Nature Neuroscience : 1157-1167 -
Chemogenetic actuator drugs impair prefrontal cortex-dependent working memory in rhesus monkeys
Upright and Baxter (2019) bioRxiv : https://doi.org/10.1101/864140 -
Binding of 5H-dibenzo[b,e][1,4]diazepine and chiral 5H-dibenzo[a,d]cycloheptene analogues of clozapine to dopamine and serotonin receptors.
Phillips et al (1994) J Med Chem 37(17) : 2686-96
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