The muscarinic acetylcholine receptor family consists of five GPCRs that mediate some
of the neurotransmission functions of acetylcholine in the CNS and the periphery. The
M1 receptor, along with the M3 and M5 receptors, signal through Gq/11 and subsequent
release of Ca++ from the ER. The M1 receptor is expressed in ganglia and mediates
depolarization of ganglia by inhibition of voltage-gated M-type K+ channels. In addition,
the M1 receptor mediates venous contraction (Caulfield and Birdsall, 1998). Chemicon’s
cloned human M1-expressing cell line is made in the Chem-1 host, which supports high
levels of recombinant M1 expression on the cell surface and contains high levels of the
promiscuous G protein Gα15 to couple the receptor to the calcium signaling pathway.
Thus, the cell line is an ideal tool for screening for antagonists of interactions between M1
and its ligands.