DREADD agonist 21
Chemical Name: 11-(1-Piperazinyl)-5H-dibenzo[b,e][1,4]diazepine
Biological ActivityPotent 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).
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
The first structure-activity relationship studies for designer receptors exclusively activated by designer drugs.
Chen et al.
ACS Chem.Neurosci., 2015;18:476
DREADD agonist 21 (C21) is an effective agonist for muscarinic-based DREADDs in vitro and in vivo.
Thompson et al.
ACS Pharmacol.Transl.Sci., 2018;
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