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Submit ReviewDREADD agonist 21
Description: Potent hM3Dq and hM4Di DREADD agonist; blood brain barrier penetrant
Alternative Names: Compound 21,C21
Chemical Name: 11-(1-Piperazinyl)-5H-dibenzo[b,e][1,4]diazepine
Purity: ≥98% (HPLC)
Biological Activity for DREADD agonist 21
DREADD agonist 21 is a potent muscarinic DREADD agonist (pEC50 values are 8.91, 8.48 and 7.77 for hM1Dq, hM3Dq and hM4Di in vitro, respectively). Exhibits > 10-fold higher affinity for hM1Dq and hM4Di compared to wild type receptors. Also displays little to no activity at wild type M3 receptors. Activates neurons expressing hM3Dq DREADDS and inhibits activity in neurons expressing hM4Di in vivo. Displays excellent brain permeability. Water soluble salt also available, DREADD agonist 21 hydrochloride (Cat. No. 6422).
Technical Data for DREADD agonist 21
| M. Wt | 278.35 |
| Formula | C17H18N4 |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 56296-18-5 |
| PubChem ID | 11818276 |
| InChI Key | JCBYXNSOLUVGTF-UHFFFAOYSA-N |
| Smiles | C1(N4CCNCC4)=NC(C=CC=C3)=C3NC2=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 DREADD agonist 21
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 27.84 | 100 | |
| ethanol | 27.84 | 100 |
Preparing Stock Solutions for DREADD agonist 21
The following data is based on the product molecular weight 278.35. 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 |
|---|---|---|---|
| 1 mM | 3.59 mL | 17.96 mL | 35.93 mL |
| 5 mM | 0.72 mL | 3.59 mL | 7.19 mL |
| 10 mM | 0.36 mL | 1.8 mL | 3.59 mL |
| 50 mM | 0.07 mL | 0.36 mL | 0.72 mL |
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Product Datasheets for DREADD agonist 21
References for DREADD agonist 21
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. 18 476 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 DREADD agonist 21, please let us know.
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Keywords: DREADD agonist 21, DREADD agonist 21 supplier, designer, receptors, drugs, DREADDs, hM3Dq, muscarinic, compound, 21, C21, Compound, Non-selective, Muscarinics, 5548, Tocris Bioscience
5 Citations for DREADD agonist 21
Citations are publications that use Tocris products. Selected citations for DREADD agonist 21 include:
James P et al (2020) Chronic postnatal chemogenetic activation of forebrain excitatory neurons evokes persistent changes in mood behavior. Elife 9 PMID: 32955432
Nathaniel et al (2020) Amygdala inhibitory neurons as loci for translation in emotional memories. Nature 586 407-411 PMID: 33029009
Smith et al (2016) DREADDS: Use and application in behavioral neuroscience. Behav Neurosci 130 137 PMID: 26913540
Peng et al (2023) Highly synchronized cortical circuit dynamics mediate spontaneous pain in mice. J Clin Invest 133 PMID: 36602876
Streamson et al (2023) The gut signals to AGRP-expressing cells of the pituitary to control glucose homeostasis. J Clin Invest 133 PMID: 36787185
Do you know of a great paper that uses DREADD agonist 21 from Tocris? Please let us know.
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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.