Description Effective agonist for muscarinic-based DREADDs in vitro and in vivo. Non-CNO chemogenetic actuator
Alternative names NSC291840 Biological Data
Perlapine is a potent agonist at muscarinic based DREADDs such as the excitatory hM3Dq, hM1Dq and inhibitory hM4Di DREADDs (pEC
50 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. Chemical Data
Chemical name 6-(4-Methyl-1-piperazinyl)-11H-dibenz[b,e]azepine
Molecular Formula C 19H 21N 3
InChiKey PWRPUAKXMQAFCJ-UHFFFAOYSA-N 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