Perlapine has been indicated to be a novel, potent and selective hM3Dq DREADD receptor agonist
Perlapine has been indicated to be a novel, potent and selective hM3Dq DREADD receptor agonist (EC50 = 2.8 nM) which also activates the inhibitory hM2Di and hM4Di Gi-DREADDs. Water soluble perlapine dihydrochloride also available.
Perlapine shows >10,000-fold selectivity for hM3Dq over hM3 muscarinic receptor.
Unlike CNO, perlapine is especially suited for translational studies.
Also acts as a sleep inducing, hypnotic agent.
Storing and Using Your Product
Soluble in DMSO (50 mM)
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) : 476-84PubMedID: 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) : 325-37PubMedID: 4695567
DREADDs for Neuroscientists.Roth Bl (2016) Neuron 89(4) : 683-94PubMedID: 26889809
Reviews & Product Guides
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