Perlapine dihydrochloride (water soluble)
Effective agonist for muscarinic-based DREADDs in vitro and in vivo. Non-CNO chemogenetic actuator. Water soluble.
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 (pEC50 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.
Storing and Using Your Product
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.
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 dihydrochloride (water soluble)
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
DREADD Agonist 21 Is an Effective Agonist for Muscarinic-Based DREADDs in Vitro and in VivoThompson et al (2018) ACS Pharmacol. Transl. Sci. Thompson et al : /acsptsci.8b00012