Human muscarinic acetylcholine receptor M3 DREADD (hM3Dq)

The human muscarinic acetylcholine receptor M3 DREADD (hM3Dq) is a genetically modified G protein-coupled receptor (GPCR) based on the human M3 muscarinic receptor. It is engineered to be unresponsive to its natural ligand, acetylcholine, but selectively activated by synthetic small molecules such as clozapine-N-oxide (CNO) or DREADD agonist 21 (C21)[7]. Upon activation by these ligands, hM3Dq couples to Gq/11 proteins, initiating a canonical Gq signaling cascade that increases intracellular calcium. This tool allows researchers to control the activity of specific cell populations in vivo or in vitro with high selectivity. It has been widely used in neuroscience, metabolic, immune, and cardiovascular research, as well as in the development of chemogenetic therapies. Its main application is experimental, but its use has provided critical insights into the roles of specific cell types in physiology and disease[7][5][3]. Note: The DREADD technology is not a natural or endogenous therapeutic target, but rather an engineered, research-only construct derived from a well-characterized native receptor[7]. The entry as written here is specific and accurate for research and synthetic biology applications.

Other names

hM3DqDREADD M3Gq-DREADDHuman muscarinic M3 DREADD

Activation by DREADD-specific synthetic agonists leads to Gq/11 signaling cascade, raising intracellular calcium, activating downstream effectors as does wild-type M3, but selectively in engineered cells[7].