Clozapine

(HB1607)

Product overview

  • Name
    Clozapine
  • Short description
    Prototypic, atypical antipsychotic, binds to both serotonin and dopamine receptors
  • Biological description

    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 antisychotic, 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.


    Water soluble version of clozapine also available

  • Biological action
    Agonist
  • Purity
    >99%
  • Citations

Properties

  • Chemical name
    8-Chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine
  • Molecular Weight
    326.83
  • Chemical structure
    Clozapine  [5786-21-0]
  • Molecular Formula
    C18H19ClN4
  • CAS Number
    5786-21-0
  • PubChem identifier
    2818
  • SMILES
    CN1CCN(CC1)C2=C3C=CC=CC3=NC4=C(N2)C=C(C=C4)Cl
  • InChi
    InChI=1S/C18H19ClN4/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
  • InChiKey
    ZUXABONWMNSFBN-UHFFFAOYSA-N
  • MDL number
    MFCD00153785
  • Appearance
    Yellow solid

Storing and Using Your Product

  • Storage instructions
    Room temperature
  • Solubility overview
    Soluble in DMSO (100 mM) and in ethanol (50 mM)
  • 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

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

    Strange 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