Deschloroclozapine (DCZ)

(HB8555)
Technical documents: SDS CoA Datasheet
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Product overview

Name Deschloroclozapine (DCZ)
Alternative names DCZ
Purity >98%
Description Potent, selective and metabolically stable hM3Dq and hM4Di muscarinic DREADD actuator.
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Deschloroclozapine (DCZ) product vial image | Hello Bio

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

Calculators

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Dilution

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Chemical Data

Purity >98%
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
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)

References are publications that support the biological activity of the product
  • 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

3 Item(s)

Publications
These publications cite the use of Deschloroclozapine (DCZ) purchased from Hello Bio:
  • Defining the Role of Locus Coeruleus Noradrenergic Neurons in the Modulation of Homeostatic Feeding

    Paul et al (2022) UCONN : Thesis

1 Item