| Bioactivity | Deschloroclozapine, a metabolite of Clozapine, is a highly potent muscarinic DREADDs agonist. Deschloroclozapine binds to DREADD receptor subtypes hM3Dq and hM4Di with Ki of 6.3 and 4.2 nM, respectively. [11C]-Deschloroclozapine is developed as a promising PET tracer for DREADD imaging[1][2][3]. | |||||||||
| Target | Ki: 6.3 nM (hM3Dq), 4.2 nM (hM4Di) | |||||||||
| Invitro | Designer Receptors Exclusively Activated by Designer Drugs (DREADD) are a chemogenetic approach for remote manipulation of neuronal activity in freely-moving animals. DREADDs comprise mutated G protein-coupled receptors (GPCRs) that do not respond to their endogenous neurotransmitter, but do respond to an otherwise “inert” exogenous substance[2]. | |||||||||
| In Vivo | Deschloroclozapine (0.3 mg/kg; intramuscularly) impairs working memory function in male rhesus macaques (aged between 5 and 6 years and weighing 5.5-7.9 kg)[3].Deschloroclozapine (0.1 mg/kg; i.m) is effective at activating DREADD receptors in vivo and reversibly inducing behavioral effects in monkeys[3]. | |||||||||
| Name | Deschloroclozapine | |||||||||
| CAS | 1977-07-7 | |||||||||
| Formula | C18H20N4 | |||||||||
| Molar Mass | 292.38 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
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| Reference | [1]. Maggs JL, et al. The metabolic formation of reactive intermediates from clozapine, a drug associated with agranulocytosis in man. J Pharmacol Exp Ther. 1995;275(3):1463-1475. [2]. Hu F, et al. 18F-labeled radiotracers for in vivo imaging of DREADD with positron emission tomography. Eur J Med Chem. 2021;213:113047. [3]. Upright NA, et al. Effect of chemogenetic actuator drugs on prefrontal cortex-dependent working memory in nonhuman primates. Neuropsychopharmacology. 2020;45(11):1793-1798. |
Deschloroclozapine
CAS: 1977-07-7 F: C18H20N4 W: 292.38
Deschloroclozapine, a metabolite of Clozapine, is a highly potent muscarinic DREADDs agonist. Deschloroclozapine binds t
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