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Data

Product overview

  • Name
    Perlapine
  • Short description
    Effective agonist for muscarinic-based DREADDs in vitro and in vivo. Non-CNO chemogenetic actuator
  • Biological description

    Perlapine 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). Water soluble form also available.


    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
  • Biological action
    Activator
  • Purity
    >98%
  • Citations

Images

Properties

  • Chemical name
    6-(4-Methyl-1-piperazinyl)-11H-dibenz[b,e]azepine
  • Molecular Weight
    291.4
  • Chemical structure
    Perlapine [1977-11-3]
  • Molecular Formula
    C19H21N3
  • CAS Number
    1977-11-3
  • PubChem identifier
    16106
  • SMILES
    CN1CCN(CC1)C2=NC3=CC=CC=C3CC4=CC=CC=C42
  • Source
    Synthetic
  • InChi
    InChI=1S/C19H21N3/c1-21-10-12-22(13-11-21)19-17-8-4-2-6-15(17)14-16-7-3-5-9-18(16)20-19/h2-9H,10-14H2,1H3
  • InChiKey
    PWRPUAKXMQAFCJ-UHFFFAOYSA-N
  • MDL number
    MFCD00242700
  • Appearance
    White solid

Storing and Using Your Product

  • Storage instructions
    Room temperature
  • Solubility overview
    Soluble in DMSO (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 Perlapine

  • 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. 10.1021 : /acsptsci.8b00012
Support & Resources

Reviews

  • Verified customer, UT Southwestern

    Our lab tested Compound 21 (DREADD agonist 21) dihydrochloride and perlapine at 1 mg/kg (i.p.) in mice and compared its effects to that of CNO and clozapine. Compound 21, perlapine, CNO and clozapine (from Hello Bio) all effectively produced the anticipated phenotype in our DREADD-Gq animals, but not in control non-DREADD animals. The effects produced with clozapine and CNO were greater than with compound 21 and perlapine, likely due to higher affinity to DREADDs. We also noticed that the effects of compound 21 and CNO were more prolonged than that of perlapine and clozapine, perhaps due to delayed retroconversion. Overall, all of the aforementioned compounds appear suitable for chemogenetics studies, providing well-controlled experiments are used