Muscarinic acetylcholine receptor

spinqualitylabelsall models Human muscarinic acetylcholine receptor M2 complex with antagonist (PDB code 5zkb) Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Function Muscarinic acetylcholine receptors (mAChR) contain 5 subtypes M1-M5. Subtypes M1, M3, M5 activate phospholipase C which leads to activation of protein kinase C. M2 and M4 inhibit adenylyl cyclase activity and activate G protein-gated potassium channels. mAChRs belong to the family of rhodopsin-like G protein coupled seven transmembrane helix receptors and perform various non-neuronal functions. Disease mAChR M1 agonists are developed for treatment of Alzheimer disease. M2 antagonists are developed for treatment of Alzheimer disease and M3 antagonists for treatment of overactive bladder and chronic obstructive pulmonary disease Structural highlights Antagonists bind to mAChR M2 at the tyrosine lid. The antagonist interacts with protein residues D103, Y104, S107, Y403 and N404. See also: G protein-coupled receptor Receptor Transmembrane (cell surface) receptors Tiotropium bromide

3D Structures of muscarinic acetylcholine receptors

Updated on 05-January-2026

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• Muscarinic acetylcholine receptor M1
  • G protein-coupled receptor – hAChR M1 (mutant) + guanine nucleotide-binding protein + scFv + transducing b chain 1 – human – Cryo EM
    
  • Receptor – hAChR M1 (mutant) + flag peptide + tiotropium
    
  • Transmembrane (cell surface) receptors – hAChR M1/endolysin + muscarinic toxin 7
    
  • Tiotropium bromide, 6zg4, 6zg9 – hAChR M1 (mutant)/endolysin + agonist
    
  • 9jea, 9uaz – hAChR M1 + atropine – Cryo EM
    
  • 9uap – hAChR M1 + guanine nucleotide-binding protein subunit alpha-11 – Cryo EM
    
  • 9ucp – hAChR M1 + guanine nucleotide-binding protein subunit alpha-11 + nanobody + iperoxo – Cryo EM
    
• Muscarinic acetylcholine receptor M2
  • 3uon, 5yc8, 5zk3, 5zk8, 5zkb, 5zkc – hAChR M2 (mutant) + antagonist
    
  • 4mqs – hAChR M2 (mutant) + nanobody + iperoxo
    
  • 4mqt – hAChR M2 (mutant) + nanobody + iperoxo + modulator
    
  • 6oik – hAChR M2 (mutant) + guanine nucleotide-binding protein + antibody fragment + transducing b chain 1 – Cryo EM
    
  • 8j8r, 8j97, 8jaf – hAChR M2 + antibody + arrestin – Cryo EM
    
  • 6u1n – hAChR M2/V2R + antibody + arrestin – Cryo EM
    
  • 7t8x, 7t90 – hAChR M2 + guanine nucleotide-binding protein + scFv + acetylcholine – Cryo EM
    
  • 7t94 – hAChR M2 + guanine nucleotide-binding protein + scFv + acetylcholine + modulator + pyridine derivative – Cryo EM
    
  • 1a11 – rAChR M2 transmembrane domain – rat - NMR
    
• Muscarinic acetylcholine receptor M3
  • 8ea0 – hAChR M3 + agonist – Cryo EM
    
  • 8e9y – hAChR M3 + guanine nucleotide-binding protein + scFv + agonist – Cryo EM
    
  • 8e9z – hAChR M3 + guanine nucleotide-binding protein + scFv + agonist + cholesterol – Cryo EM
    
  • 8e9w – hAChR M3 + guanine nucleotide-binding protein + scFv + piperazine derivative – Cryo EM
    
  • 4daj – rAChR M3
    
  • 4u14, 4u15 – rAChR M3 + tiotropium
    
  • 4u16, 5zhp – rAChR M3 + inhibitor
    
• Muscarinic acetylcholine receptor M4
  • 5dsg – hAChR M4 + tiotropium
    
  • 6kp6 – hAChR M4 (mutant)
    
  • 6d9h, 7ld4 – hAChR M4/adenosine receptor+ guanine nucleotide-binding protein + agonist – Cryo EM
    
  • 7ld3 – hAChR M4/adenosine receptor+ guanine nucleotide-binding protein + ligand – Cryo EM
    
  • 7v69 – hAChR M4 + guanine nucleotide-binding protein + scFv – Cryo EM
    
  • 7trk – hAChR M4 + guanine nucleotide-binding protein + scFv + agonist – Cryo EM
    
  • 7trs – hAChR M4 + guanine nucleotide-binding protein + scFv + acetylcholine – Cryo EM
    
  • 7trq – hAChR M4 + guanine nucleotide-binding protein + scFv + agonist + modulator – Cryo EM
    
  • 7v6a – hAChR M4 + guanine nucleotide-binding protein + scFv + piperidine derivative – Cryo EM
    
  • 8fx5 – hAChR M4 + guanine nucleotide-binding protein + scFv + drug – Cryo EM
    
  • 9kwx, 9kzk – hAChR M4/anaphylatoxin + guanine nucleotide-binding protein + scFv + anaphylatoxin – Cryo EM
    
  • 9kv6, 9kv8 – hAChR M4/anaphylatoxin + guanine nucleotide-binding protein + scFv + VGF peptide – Cryo EM
    
  • 9l0h – hAChR M4/anaphylatoxin + guanine nucleotide-binding protein + scFv – Cryo EM
    
  • 9kx6 – hAChR M4/anaphylatoxin + guanine nucleotide-binding protein + complement C5 + scFv – Cryo EM
    
  • 9umj, 9umx – hAChR M4/anaphylatoxin + guanine nucleotide-binding protein + EP54 ligand + scFv – Cryo EM
    
  • 9umr – hAChR M4/anaphylatoxin + guanine nucleotide-binding protein + C5A-PEP ligand + scFv – Cryo EM
    
  • 9kug, 9kxs, 9kz2, 9kz8 – hAChR M4/anaphylatoxin + guanine nucleotide-binding protein + EP67 ligand + scFv – Cryo EM
    
  • 9kut – hAChR M4/anaphylatoxin + guanine nucleotide-binding protein + JR14a + scFv – Cryo EM
    
  • 9kwg – hAChR M4/anaphylatoxin + guanine nucleotide-binding protein + anaphylatoxin + scFv – Cryo EM
    
  • 9kvp – hAChR M4/anaphylatoxin + guanine nucleotide-binding protein + ligand + scFv – Cryo EM
    
  • 9iqs – hAChR M4/cytochrome b562 + muscarinic toxin 3 – Cryo EM
    
  • 7t96, 7trp – hAChR M4 + guanine nucleotide-binding protein + scFv + acetylcholine + modulator + pyridine derivative – Cryo EM
    
  • 7v68 – hAChR M4 + guanine nucleotide-binding protein + scFv + agonist + modulator + pyridine derivative – Cryo EM
    
  • 8e9x – hAChR M4 (mutant) + guanine nucleotide-binding protein + scFv + agonist – Cryo EM
    
• Muscarinic acetylcholine receptor M5
  • 6ol9 – hAChR M5 + tiotropium
    
  • 9ejz – hAChR M5 + guanine nucleotide-binding protein + nanobody + scFv + acetylcholine – Cryo EM
    
  • 9ek0 – hAChR M5 + guanine nucleotide-binding protein + iperoxo – Cryo EM
    

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