Catalog No. size PriceQuantity
M7158-2 2mg solid $121
M7158-10 10mg solid $476


Deschloroclozapine is a high affinity and highly potent activator of muscarinic DREADDs. It is a derivative of clozapine, and exhibits 100-fold greater affinity for hM3Dq and hM4Di compared to clozapine N-oxide, and 50-fold greater affinity compared to DREADD agonist 21. Deschloroclozapine displays low 'off-target' receptor binding and rapid binding and activation of hM3Dq and hM4Di in mice and non-human primates. It also induces spatial memory deficits in non-human primates expressing hM4Di in the prefrontal cortex.

Product information

CAS Number: 1977-07-7

Molecular Weight: 292.38

Formula: C18H20N4




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

Dopamine serotonin antagonist-1

11-(4-Methylpiperazin-1-yl)-5H-dibenzo[b, e][1, 4]diazepine

BRN 0761696


6-(4-methylpiperazin-1-yl)-11H-benzo[b][1, 4]benzodiazepine

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


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












5-25-11-00363 (Beilstein Handbook Reference)

5H-Dibenzo[b, e][1, 4]diazepine, 11-(4-methyl-1-piperazinyl)-

Chemical Name: 11-(4-methylpiperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepine

Smiles: CN1CCN(CC1)C1=NC2=CC=CC=C2NC2=CC=CC=C21


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

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

Deschloroclozapine has greater potencies for DREADDs than previous agonists in vitro. Deschloroclozapine is a potent agonist for hM3Dq with an EC50=0.13 nM. Deschloroclozapine is also a potent agonist for hM4Di with an EC50=0.081 nM. Deschloroclozapine is a potent and selective agonist for hM3Dq and hM4Di, it does not display significant agonistic activity for any of the 318 tests wild-type GPCRs at <10 nM.

In Vivo:

Deschloroclozapine (100 μg/kg; i.v.) exhibits good brain concentration profiles and biostability. Pharmacokinetic studies confirmed that Deschloroclozapine is rapidly accumulated in mouse brains and monkey CSF, while its metabolites are negligible. Deschloroclozapine (1 μg/kg; i.p.) selectively and rapidly enhances neuronal activity via hM3Dq-DREADD in vivo, Deschloroclozapine can also be utilized for in vivo neuronal silencing by activating hM4Di, an inhibitory DREADD[1]. Deschloroclozapine (1-100 μg/kg; i.v.) selectively induces hM3Dq-mediated metabolic activity. Deschloroclozapine (100 μg/kg; i.m.) selectively induces behavioral deficits in hM4Di-expressing monkeys.


  1. Upright NA, Baxter MG. Effect of chemogenetic actuator drugs on prefrontal cortex-dependent working memory in nonhuman primates. Neuropsychopharmacology. 2020 Oct;45(11):1793-1798. doi: 10.1038/s41386-020-0660-9. Epub 2020 Mar 19. PMID: 32193513.
  2. Maggs JL, Williams D, Pirmohamed M, Park BK. The metabolic formation of reactive intermediates from clozapine, a drug associated with agranulocytosis in man. J Pharmacol Exp Ther. 1995 Dec;275(3):1463-75. PMID: 8531117.

Products are for research use only. Not for human use.

Payment & Security

American Express Diners Club Discover JCB Mastercard PayPal Venmo Visa

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed