DREADD Agonists Small Molecules and Peptides

DREADD Mechanism of Action

The first DREADDs to be developed were derived from human muscarinic acetylcholine receptors (mAChRs) and termed hM1-5. These receptors have mutations in their orthosteric binding site, abolishing their affinity for the endogenous ligand ACh, while rendering them responsive to small molecule DREADD ligands, such as Clozapine-N-oxide (CNO, Cat. No. 4936) or Deschloroclozapine (DCZ, Cat. No. 7193).

The effect of ligand binding depends on the G protein-coupling of the ...