Structure of the human M2 muscarinic acetylcholine receptor bound to an antagonist (original) (raw)

The parasympathetic limb of the autonomic nervous system regulates the activity of multiple organ systems. Muscarinic receptors are G protein coupled receptors (GPCRs) that mediate the response to acetylcholine released from parasympathetic nerves. 1-5 Their role in the unconscious regulation of organ and central nervous system function makes them potential therapeutic targets for a broad spectrum of diseases. The M 2 muscarinic acetylcholine receptor (M 2 receptor) is essential for the physiologic control of cardiovascular function through activation of G proteincoupled inwardly-rectifying potassium channels, and is of particular interest because of its extensive pharmacological characterization with both orthosteric and allosteric ligands. Here we