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Submit ReviewPerlapine
Description: Potent hM3Dq and hM4Di DREADD agonist in vitro
Chemical Name: 6-(4-Methyl-1-piperazinyl)-11H-dibenz[b,e]azepine
Purity: ≥99% (HPLC)
Biological Activity for Perlapine
Perlapine is a potent muscarinic DREADD agonist (pEC50 values are 8.38, 8.08 and 7.27 for hM1Dq, hM3Dq and hM4Di in vitro, respectively). Exhibits >10,000-fold selectivity for hM3Dq over hM3 receptors.
Technical Data for Perlapine
| M. Wt | 291.39 |
| Formula | C19H21N3 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 1977-11-3 |
| PubChem ID | 16106 |
| InChI Key | PWRPUAKXMQAFCJ-UHFFFAOYSA-N |
| Smiles | CN(CC4)CCN4C1=NC(C=CC=C3)=C3CC2=C1C=CC=C2 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Perlapine
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 14.57 | 50 | |
| water | 1.46 | 5 with gentle warming |
Preparing Stock Solutions for Perlapine
The following data is based on the product molecular weight 291.39. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 6.86 mL | 34.32 mL | 68.64 mL |
| 2.5 mM | 1.37 mL | 6.86 mL | 13.73 mL |
| 5 mM | 0.69 mL | 3.43 mL | 6.86 mL |
| 25 mM | 0.14 mL | 0.69 mL | 1.37 mL |
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Product Datasheets for Perlapine
References for Perlapine
References are publications that support the biological activity of the product.
Chen et al (2015) The first structure-activity relationship studies for designer receptors exclusively activated by designer drugs. ACS Chem.Neurosci. 6 476 PMID: 25587888
Thompson et al (2018) DREADD agonist 21 (C21) is an effective agonist for muscarinic-based DREADDs in vitro and in vivo. ACS Pharmacol.Transl.Sci. 1 61 PMID: 30868140
If you know of a relevant reference for Perlapine, please let us know.
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Keywords: Perlapine, Perlapine supplier, Perlapine, potent, selective, hM3Dq, DREADD, agonists, antagonism, designer, receptors, drugs, muscarinic, activators, chemogenetics, DREADDs, Non-selective, Muscarinics, 5549, Tocris Bioscience
1 Citation for Perlapine
Citations are publications that use Tocris products. Selected citations for Perlapine include:
Weston et al (2019) Olanzapine: A potent agonist at the hM4D(Gi) DREADD amenable to clinical translation of chemogenetics. Sci Adv. 5 PMID: 31001591
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Chemogenetics Research Bulletin
Produced by Tocris, the chemogenetics research bulletin provides an introduction to chemogenetic methods to manipulate neuronal activity. It outlines the development of RASSLs, DREADDs and PSAMs, and the use of chemogenetic compounds. DREADD ligands and PSEMs available from Tocris are highlighted.
Allosteric GPCR Pharmacology Poster
G protein-coupled receptors (GPCRs) are intrinsically allosteric proteins. This poster provides insights into allosteric mechanisms of GPCR biology, highlighting key facets of GPCR allostery and therapeutic applications of allosteric modulators.
GPCR Efficacy and Biased Agonism Poster
GPCRs can interact with multiple distinct transducers or regulatory proteins and these can be preferentially engaged in an agonist-specific manner giving rise to biased agonism. This poster discusses cutting edge GPCR signaling pharmacology and highlights therapeutic applications of biased agonism.