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SML3651

Sigma-Aldrich

Deschloroclozapine

≥98% (HPLC)

Sinónimos:

11-(4-Methyl-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine, DCZ

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About This Item

Fórmula empírica (notación de Hill):
C18H20N4
Número de CAS:
1977-07-7
Peso molecular:
292.38
MDL number:
MFCD01730958
UNSPSC Code:
12352200
NACRES:
NA.21

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Biochem/physiol Actions

Deschloroclozapine (DCZ) is a potent and selective DREADDs (Designer Receptors Exclusively Activated by Designer Drugs) agonist (hM3Dq/hM4Di Ki = 6.3/4.2 nM vs hM3/hM4 Ki = 230/210 nM; hM3Dq/hM4Di EC50 = 130/81 nM by celluar BRET assays) with much greater potency than CNO and C21. DCZ selectively stimulates DREADDs, but not non-DREADDs, cells (Ca2+ EC50 = 2.3 nM/hM3Dq, cAMP IC50 = 0.0048 nM/hM4Di, β-arrestin recruitment EC50 = 0.63 nM/hM3Dq & 0.048 nM/hM4Di). DCZ enhances neuronal activity in hM3Dq mice (1 μg/kg i.p.) & monkeys (1-3 μg/kg i.v.) and induces spatial working memory deficits in hM4Di monkeys (100 μg/kg i.m.) in vivo.
Potent muscarinic-based DREADDs (Designer Receptors Exclusively Activated by Designer Drugs) ligand with in vivo CNS potency.

pictograms

Skull and crossbones
GHS06

signalword

Danger

hcodes

H301

Hazard Classifications

Acute Tox. 3 Oral

Storage Class

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Nicholas A Upright et al.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, 45(11), 1793-1798 (2020-03-21)
The most common chemogenetic neuromodulatory system, designer receptors exclusively activated by designer drugs (DREADDs), uses a non-endogenous actuator ligand to activate a modified muscarinic acetylcholine receptor that is insensitive to acetylcholine. It is crucial in studies using these systems to
Yuji Nagai et al.
Nature neuroscience, 23(9), 1157-1167 (2020-07-08)
The chemogenetic technology designer receptors exclusively activated by designer drugs (DREADDs) afford remotely reversible control of cellular signaling, neuronal activity and behavior. Although the combination of muscarinic-based DREADDs with clozapine-N-oxide (CNO) has been widely used, sluggish kinetics, metabolic liabilities and

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