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Perlapine dihydrochloride (water soluble)

(HB6126)
Data

Product overview

  • Name
    Perlapine dihydrochloride (water soluble)
  • Short description
    Effective agonist for muscarinic-based DREADDs in vitro and in vivo. Water soluble.
  • Biological description

    Perlapine dihdrochloride is the water soluble of perlapine which is a potent agonist at muscarinic based DREADDs such as the excitatory hM3Dq, hM1Dq and inhibitory hM4Di DREADDs (pEC50 values are 8.08, 8.38 and 7.27 at hM3Dq, hM1Dq and hM4Di respectively).


    Perlapine exhibits >10,000-fold selectivity for hM3Dq over wildtype hM3 and interacts with wildtype hM1 and hM4 receptors with relatively low affinity. Perlapine lacks agonist activity at wild type receptors.


    It has been reported that perlapine does not undergo back metabolism to clozapine.


    Perlapine also acts as a sleep inducing, hypnotic agent.


    CNO dihydrochloride (water soluble), Clozapine N-oxide (CNO) freebase, Compound 21, Salvinorin B (SalB) and perlapine freebase also available.

  • Alternative names
    NSC291840 dihydrochloride
  • Biological action
    Activator
  • Purity
    >98%
  • Citations

Properties

  • Chemical name
    6-(4-Methyl-1-piperazinyl)-11H-dibenz[b,e]azepine dihydrochloride
  • Molecular Weight
    360.3
  • Chemical structure
    Perlapine hydrochloride
  • Molecular Formula
    C19H21N3.2HCl
  • SMILES
    CN1CCN(CC1)C2=NC3=CC=CC=C3CC4=CC=CC=C42.Cl.Cl
  • Source
    Synthetic
  • Appearance
    White solid

Storing and Using Your Product

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

  • 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 Perlapine dihydrochloride (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
  • 6-(4-Methyl-1-piperazinyl)morphanthridine (Perlapine), a new tricyclic compound with sedative and sleep-promoting properties. A pharmacological study.

    Stille et al (1973) Psychopharmacologia 24(4) : 325-37
    PubMedID: 4695567
  • DREADDs for Neuroscientists.

    Roth Bl (2016) Neuron 89(4) : 683-94
    PubMedID: 26889809
  • DREADD Agonist 21 Is an Effective Agonist for Muscarinic-Based DREADDs in Vitro and in Vivo

    Thompson et al (2018) ACS Pharmacol. Transl. Sci. Thompson et al : /acsptsci.8b00012
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