Acetylcholine Muscarinic Receptors

Muscarinic receptors are widely distributed throughout the body and control distinct functions according to location and subtype (M1 - M5).They are predominantly expressed in the parasympathetic nervous system where they exert both inhibitory and excitatory effects.

Acetylcholine Muscarinic Receptor Target Files

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Muscarinic receptor agonists and antagonists could prove useful in the research and treatment of a wide range of central nervous system diseases including Alzheimer's disease and Parkinson's disease.

The table below summarizes the properties of muscarinic receptors and includes affinity values of some key muscarinic receptor-selective ligands available from Tocris.

Receptor Subtype M1 M2 M3 M4 M5
Transduction Mechanism ↑PLC (Gq/11) ↓Adenylyl Cyclase (Gi/o) ↑PLC (Gq/11) ↓Adenylyl Cyclase (Gi/o) ↑PLC (Gq/11)
Primary Distribution Neocortex, hippocampus, neostriatum, salivary glands, eye, heart Brain, heart, smooth muscle, salivary glands Smooth muscle, exocrine glands, brain, autonomic ganglia, salivary glands Neostriatum, cortex, hippocampus, autonomic ganglia Substantia nigra, pars compacta, ventral tegmental area, hippocampus
Tissue Function Learning and memory, neuromodulation, M-current inhibition Bradycardia, smooth muscle contraction, antinociception, hyperthermia, ↓ neurotransmitter release (presynaptic) Smooth muscle contraction, gland secretion, ↓ neurotransmitter release (presynaptic) Regulation of dopamine D1 stimulated locomotor activity Unknown

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