Muscarinic acetylcholine M1 receptor (M1 mAChR)

The muscarinic acetylcholine M1 receptor (M1 mAChR) is a G protein-coupled receptor primarily coupled to Gq/11 proteins, leading to activation of phospholipase C, increased IP3, and elevated intracellular calcium levels. Predominantly expressed in the brain, it plays a crucial role in cognitive functions, learning, and memory. It is also found in exocrine glands and autonomic ganglia, mediating secretion and slow EPSPs, respectively. Due to its involvement in cognitive processes, M1 mAChR is a therapeutic target for Alzheimer's disease. Drug development focuses on subtype-selective positive allosteric modulators (PAMs) and negative allosteric modulators (NAMs) targeting the extracellular vestibule (ECV) to improve cognition while minimizing side effects from peripheral muscarinic receptor activation. Antagonism of M1 receptors can cause delirium-like states.

Other names

CHRM1Cholinergic Receptor Muscarinic 1M1 Receptor

Activation of Gq/11 proteins, leading to activation of phospholipase C, increased inositol trisphosphate (IP3), and elevated intracellular calcium levels. In some tissues, can also interact with Gi or Gs proteins affecting cAMP levels. Allosteric modulation via PAMs/NAMs.