DREADD agonist 21
Chemical Name: 11-(1-Piperazinyl)-5H-dibenzo[b,e][1,4]diazepine
Purity: ≥98%
Biological Activity
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
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.
Background References
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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;1:61
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Citations for DREADD agonist 21
The citations listed below are publications that use Tocris products. Selected citations for DREADD agonist 21 include:
5 Citations: Showing 1 - 5
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Highly synchronized cortical circuit dynamics mediate spontaneous pain in mice.
Authors: Peng Et al.
J Clin Invest 2023;133
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The gut signals to AGRP-expressing cells of the pituitary to control glucose homeostasis.
Authors: Streamson Et al.
J Clin Invest 2023;133
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Chronic postnatal chemogenetic activation of forebrain excitatory neurons evokes persistent changes in mood behavior.
Authors: James P Et al.
Elife 2020;9
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Amygdala inhibitory neurons as loci for translation in emotional memories.
Authors: Nathaniel Et al.
Nature 2020;586:407-411
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DREADDS: Use and application in behavioral neuroscience.
Authors: Smith Et al.
Behav Neurosci 2016;130:137
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