1. GPCR/G Protein
    Neuronal Signaling
  2. mAChR
  3. Deschloroclozapine

Deschloroclozapine 

Cat. No.: HY-42110 Purity: 99.79%
Handling Instructions

Deschloroclozapine is a potent, high affinity, selective, metabolically stable agonist of muscarinic-based DREADDs. Deschloroclozapine inhibites [3H]quinuclidinyl benzilate (QNB) binding to hM3Dq and hM4Di with Ki of 6.3 and 4.2 nM. Deschloroclozapine is reported with utility in both mice and non-human primates for a variety of applications.

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Deschloroclozapine Chemical Structure

Deschloroclozapine Chemical Structure

CAS No. : 1977-07-7

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Description

Deschloroclozapine is a potent, high affinity, selective, metabolically stable agonist of muscarinic-based DREADDs. Deschloroclozapine inhibites [3H]quinuclidinyl benzilate (QNB) binding to hM3Dq and hM4Di with Ki of 6.3 and 4.2 nM. Deschloroclozapine is reported with utility in both mice and non-human primates for a variety of applications[1].

IC50 & Target

Ki: 6.3 nM (hM3Dq), 4.2 nM (hM4Di)[1]

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[1].
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[1].

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[1].
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[1].
Deschloroclozapine (100 μg/kg; i.m.) selectively induces behavioral deficits in hM4Di-expressing monkeys[1].

Animal Model: Macaque monkey; 2.8-8.0 kg; age 3-10 years[1]
Dosage: 10, 100, 1000, 10000 μg/kg
Administration: I.v. bolus injection
Result: Required the dose for 50% occupancy (ED50) for Deschloroclozapine was 25 μg/kg.
Animal Model: Macaque monkey; 2.8-8.0 kg; age 3-10 years[1]
Dosage: 100 μg/kg (Pharmacokinetic Analysis)
Administration: I.v. injection
Result: Provided a sufficient concentration of Deschloroclozapine by a low systemic dose of Deschloroclozapine to be available for hM4Di-DREADD binding in vivo for at least for 2 h without the production of metabolites in monkeys.
Animal Model: Wild-type C57BL/6j mice; male; age >12 weeks[1]
Dosage: 100 μg/kg (Pharmacokinetic Analysis)
Administration: I.p. administration
Result: Diminished rapidly of Deschloroclozapine concentration and were undetectable at 2 h in either brain tissue or CSF.
The amount of the desmethyl metabolite C21 in CSF was negligible.
Animal Model: HM3Dq monkeys and non-DREADD monkeys[1]
Dosage: 1, 3, 100 μg/kg (Pharmacokinetic Analysis)
Administration: I.v. injection
Result: Increased of FDG uptaking after Deschloroclozapine administration occurred exclusively at the hM3Dq-positive area.
Animal Model: Monkeys received multiple injections of an AAV-vector carrying hM4Di genes[1]
Dosage: 100 μg/kg (Pharmacokinetic Analysis)
Administration: I.m. administration
Result: Enabled a rapidly and reversibly-induced behavioral change through activating muscarinic-based DREADDs without significant side effects.
Molecular Weight

292.38

Formula

C₁₈H₂₀N₄

CAS No.

1977-07-7

SMILES

CN1CCN(C2=NC3=CC=CC=C3NC4=CC=CC=C42)CC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (342.02 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4202 mL 17.1010 mL 34.2021 mL
5 mM 0.6840 mL 3.4202 mL 6.8404 mL
10 mM 0.3420 mL 1.7101 mL 3.4202 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (8.55 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (8.55 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.55 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

DeschloroclozapinemAChRMuscarinic acetylcholine receptormuscarinic-basedDREADDshM3DqhM4DiInhibitorinhibitorinhibit

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Deschloroclozapine
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