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生物化学的/生理学的作用
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.
シグナルワード
Danger
危険有害性情報
危険有害性の分類
Acute Tox. 3 Oral
保管分類コード
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK
WGK 3
引火点(°F)
Not applicable
引火点(℃)
Not applicable
適用法令
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Jan Code
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試験成績書(COA)
Journal of neuroscience methods, 380, 109679-109679 (2022-08-02)
Chemogenetics is a powerful tool to study the role of specific neuronal populations in physiology and diseases. Of particular interest, in mice, acute and specific activation of parafacial zone (PZ) GABAergic neurons expressing the Designer Receptors Activated by Designer Drugs
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
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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