Compound 21 (DREADD agonist 21) hydrochloride (water soluble)

(HB6124)

Product overview

  • Name
    Compound 21 (DREADD agonist 21) hydrochloride (water soluble)
  • Short description
    Highly potent hM3Dq DREADD agonist. Water soluble.
  • Biological description

    Compound 21 (DREADD agonist 21) hydrochloride is a water soluble analog of clozapine N-oxide (CNO). Free base also available.


    Compound 21 (DREADD agonist 21) is a highly potent agonist at the excitatory hM3Dq DREADD (EC50 = 1.7 nM) which shows high selectivity for activating hM3Dq compared to the native hM3 muscarinic receptor and other GPCRs.


    Compound 21 has minimal off-target activity. There are indications that Compound 21 cannot be metabolized via normal routes to clozapine (or any related compound) and that Compound 21 has equivalent potency in vivo when compared with clozapine N-oxide.

    Unpublished data indicates that Compound 21 (DREADD agonist 21) activates the inhibitory hM4D DREADD.

    Unpublished data also suggests using a dose of 3mg/kg in rat models.


    Compound 21 therefore represents an alternative to CNO.

  • Purity
    >98%
  • Citations

Images

Properties

  • Chemical name
    11-(1-Piperazinyl)-5H-dibenzo[b,e][1,4]diazepine dihydrochloride
  • Molecular Weight
    352.29
  • Chemical structure
    Compound 21 hydrochloride
  • Molecular Formula
    C17H18N4.2HCl
  • SMILES
    C1CN(CCN1)C2=NC3=CC=CC=C3NC4=CC=CC=C42.Cl.Cl
  • Source
    Synthetic
  • Appearance
    Yellow solid

Storing and Using Your Product

  • Storage instructions
    RT (desiccate)
  • Solubility overview
    Soluble in water (100mM)
  • Handling
    Hydroscopic solid, 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.
  • 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 Compound 21 (DREADD agonist 21) hydrochloride (water soluble)

  • The first structure-activity relationship studies for designer receptors exclusively activated by designer drugs.

    Chen et al (2015) ACS Chem Neurosci 6(3) : 476-84
    PubMedID: 25587888
  • Optogenetic approaches for dissecting neuromodulation and GPCR signaling in neural circuits.

    Spangler and Bruchas (2017) Curr Opin Pharmacol 32(4) : 56-70.
    PubMedID: 27875804
  • Clozapine N-Oxide Administration Produces Behavioral Effects in Long-Evans Rats: Implications for Designing DREADD Experiments.

    MacLaren et al (2016) eNeuro 3(5) : 0219-16
    PubMedID: 27822508
  • New non-CNO actuators for DREADDs

    Roth Bl (2015) Blog : N/A