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Clozapine dihydrochloride (water soluble)

(HB6129)
Data

Product overview

  • Name
    Clozapine dihydrochloride (water soluble)
  • Short description
    Water soluble prototypic, atypical antipsychotic. Binds to both serotonin and dopamine receptors.
  • Biological description

    Water soluble clozapine is a prototypic, atypical antipsychotic which binds to both serotonin and dopamine receptors (Ki values are 35, 83 and 22, 250 and 141 nM at D2, D3 and D4, D5, D1 and 12.6 and 13.2 nM at 5-HT2A and 5-HT2C receptors respectively) and also shows activity at other receptors.


    Clozapine shows high BBB permeability and is active in vivo. It shows antipsychotic, antidepression and anxiolytic activites.


    Recently, clozapine (which CNO rapidly coverts to) has been indicated to show high DREADD (hM3Dq and hM4Di) affinity and potency. Subthreshold clozapine injections are indicated to induce preferential DREADD-mediated behaviors.


    Clozapine also available

  • Biological action
    Agonist
  • Purity
    >98%
  • Customer comments

    I am very pleased with this product: Clozapine dihydrochloride (clozapine-2HCl). It dissolves in saline (0.9% NaCl) well and produces the expected biological effects when injected into the mouse. Its water solubility is highly useful because the free base clozapine does not dissolve in water/saline, limiting its use in intact animals. Verified customer, UTHSC

  • Citations

Properties

  • Chemical name
    8-Chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine dihydrochloride
  • Molecular Weight
    399.75
  • Chemical structure
    Clozapine hydrochloride [54241-01-9]
  • Molecular Formula
    C18H19N4 · 2HCl
  • CAS Number
    54241-01-9
  • PubChem identifier
    148669
  • SMILES
    CN1CCN(CC1)C2=C3C=CC=CC3=NC4=C(N2)C=C(C=C4)Cl.Cl
  • Source
    Synthetic
  • InChi
    InChI=1S/C18H19ClN4.ClH/c1-22-8-10-23(11-9-22)18-14-4-2-3-5-15(14)20-16-7-6-13(19)12-17(16)21-18;/h2-7,12,21H,8-11H2,1H3;1H
  • InChiKey
    VFDNENKXDGAOSN-UHFFFAOYSA-N
  • Appearance
    Orange solid

Storing and Using Your Product

  • Storage instructions
    -20°C.
  • Solubility overview
    Soluble in water (100 mM). Always store solutions at -20°C.
  • Handling

    Storage of solid

    • Store at -20°C.
    • Please note that the compound is a hydroscopic solid and contact with air may cause material to become sticky. Product performance should not be affected but we recommend storing the material in a sealed jar.

    Storage of solutions

    • Make up solutions and use immediately.
    • If storage of solutions is required, you should aliquot out the solution into tightly sealed vials and store at -20°C and store these for up to one month.
    • Allow the product to equilibrate to RT for at least one hour before opening and using.

    • Storage of solutions at room temperature

    • We recommend only keeping solutions at room temperature (25°C) for a few days as our studies have shown that after 96 hours the purity of the compound in solution drops to ~96% and will continue to drop over time.
  • Important
    This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use

References for Clozapine dihydrochloride (water soluble)

  • Antipsychotic drugs: importance of dopamine receptors for mechanisms of therapeutic actions and side effects.

    Sunahara RK et alStrange PG (2001) Pharmacol Rev 53(1) : 119-33.
    PubMedID: 11171942
  • Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1.

    Sunahara RK et al (1991) Nature 350(6319) : 614-9.
    PubMedID: 1826762
  • Differential regulation of rat 5-HT2A and 5-HT2C receptors after chronic treatment with clozapine, chlorpromazine and three putative atypical antipsychotic drugs.

    Kuoppamã?ki M et al (1995) Neuropsychopharmacology 13(2) : 139-50.
    PubMedID: 8597525
  • Chemogenetics revealed: DREADD occupancy and activation via converted clozapine.

    Gomez et al (2017) Science 357(6350) : 503-507
    PubMedID: 28774929
Support & Resources

Reviews

  • Verified customer, Cardiff University

    Fantastic product. Readily dissolves in saline or PBS, which is not the case for freebase clozapine (which is a real challenge to dissolve). We have successfully used clozapine dihydrocloride to activate DREADDS in rats.
  • Verified customer, UTHSC

    I am very pleased with this product: Clozapine dihydrochloride (clozapine-2HCl). It dissolves in saline (0.9% NaCl) well and produces the expected biological effects when injected into the mouse. Its water solubility is highly useful because the free base clozapine does not dissolve in water/saline, limiting its use in intact animals.