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
The table below summarizes the properties of muscarinic receptors and includes affinity values of some key muscarinic receptor-selective ligands available from Tocris.
|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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Potent, selective LRRK2 inhibitor
Tocris is the first to launch GSK2578215A, licensed from GlaxoSmithKline, for the study of Parkinson's Disease.