Drug intelligence / Profile preview

deschloroclozapine

Development stage
Preclinical
Modality
Small Molecules
Administration
Intraperitoneal, Intramuscular, Oral, Subcutaneous
01

Overview

Deschloroclozapine is a potent, highly selective, and metabolically stable small molecule agonist of muscarinic DREADDs (Designer Receptors Exclusively Activated by Designer Drugs), particularly targeting hM3Dq and hM4Di receptors[1][4][8][10]. It enables rapid, reversible, and remote modulation of neuronal activity and behavior in animal models, and features greater potency and selectivity over other DREADD ligands such as clozapine-N-oxide (CNO) or DREADD agonist 21, with substantially lower off-target binding[4][7][8][10]. Deschloroclozapine rapidly penetrates the brain following systemic administration, allowing effective chemogenetic activation or inhibition of genetically modified neuronal populations. Developed primarily as a research tool, it is not approved or indicated for human therapeutic use[2][8]. The compound is a metabolite of clozapine and has been widely used in preclinical neuroscience studies to probe neural circuit function in vivo in rodents and non-human primates[1][3][4][10].

Other names
deschloroclozapine dihydrochlorideDREADD DCZ dihydrochloride
02

Targets

hM4Di (Human muscarinic acetylcholine receptor M4 designer receptor exclusively activated by designer drugs)hM3Dq (Human muscarinic acetylcholine receptor M3 DREADD)

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