Perlapine

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Cat.No. 5549 - Perlapine | C19H21N3 | CAS No. 1977-11-3
Description: Potent muscarinc DREADD agonist
Chemical Name: 6-(4-Methyl-1-piperazinyl)-11H-dibenz[b,e]azepine
Purity: ≥99% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

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

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 14.57 50
water 1.46 5 with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 291.39. Batch specific molecular weights may vary from batch to batch due to solvent 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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References

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.


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Citations for Perlapine

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Literature in this Area

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Chemogenetics

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.