Perlapine

(HB4889)
Technical documents: SDS CoA Datasheet

Product overview

Name Perlapine
Description Effective agonist for muscarinic-based DREADDs in vitro and in vivo. Non-CNO chemogenetic actuator
Alternative names NSC291840
Purity >98%
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Perlapine vial

Biological Data

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.

Solubility & Handling

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.

Calculators

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Chemical Data

Chemical name 6-(4-Methyl-1-piperazinyl)-11H-dibenz[b,e]azepine
Molecular Weight 291.4
Chemical structure Perlapine [1977-11-3] Chemical Structure
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

References for Perlapine

References are publications that support the biological activity of the product
  • DREADDs: The Power of the Lock, the Weakness of the Key. Favoring the Pursuit of Specific Conditions Rather than Specific Ligands.

    Goutaudier et al (2019) eNeuro 6 : (5)
  • 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
  • DREADDs for Neuroscientists.

    Roth Bl (2016) Neuron 89(4) : 683-94
  • 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
  • 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