Perlapine dihydrochloride (water soluble)
(HB6126) Product overview
Name Perlapine dihydrochloride (water soluble)
Alternative names NSC291840 dihydrochloride
Description Effective agonist for muscarinic-based DREADDs in vitro and in vivo. Non-CNO chemogenetic actuator. Water soluble. Biological Data
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 (pEC
50 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.
Stability Studies For more info on the stability of water-soluble DREADD ligands in solution, please see the following guides: Solubility & Handling
Storage instructions -20°C
Solubility overview Soluble in water (100 mM). Always store solutions at -20°C.
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 Chemical Data
Chemical name 6-(4-Methyl-1-piperazinyl)-11H-dibenz[b,e]azepine dihydrochloride
Molecular Formula C 19H 21N 3.2HCl
SMILES CN1CCN(CC1)C2=NC3=CC=CC=C3CC4=CC=CC=C42.Cl.Cl References for Perlapine dihydrochloride (water soluble)
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. Thompson et al : /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