Compound 21 (DREADD agonist 21)
Compound 21 has been indicated to be a highly potent hM3Dq DREADD agonist.
Compound 21 (DREADD agonist 21) ihas been indicated to be a highly potent agonist at the excitatory hM3Dq DREADD (EC50 = 1.7 nM) and shows high selectivity for activating hM3Dq compared to the native hM3 muscarinic receptor and other GPCRs.
There are indications that Compound 21 cannot be metabolized via normal routes to clozapine (or any related compound), has minimal off-target activity and has equivalent potency in vivo when compared with clozapine N-oxide (CNO).
Unpublished data indicates that Compound 21 (DREADD agonist 21) activates the inhibitory hM4D DREADD.
Unpublished data also suggests using a dose of 3mg/kg in rat models.
Data from a poster presented at SfN by the Michaelides group indicates that Compound 21 has lower binding affinity for DREADDs compared to clozapine and that Compound 21 induces behavioural effects in transgenic mice. 1mg/kg doses were used. High doses (10mg/kg) may cause sedation.
Compound 21 may therefore represent an alternative to CNO.
Storing and Using Your Product
Soluble in DMSO (100mM) and in ethanol (100mM)
This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use
References for Compound 21 (DREADD agonist 21)
The first structure-activity relationship studies for designer receptors exclusively activated by designer drugs.Chen et al (2015) ACS Chem Neurosci 6(3) : 476-84PubMedID: 25587888
Optogenetic approaches for dissecting neuromodulation and GPCR signaling in neural circuits.Spangler and Bruchas (2017) Curr Opin Pharmacol 32 : 56-70.PubMedID: 27875804
Clozapine N-Oxide Administration Produces Behavioral Effects in Long-Evans Rats: Implications for Designing DREADD Experiments.MacLaren et al (2016) eNeuro 3(5) : 0219-16PubMedID: 27822508
New non-CNO actuators for DREADDsRoth Bl (2015) Blog : N/A