Chronic pain represents a research field on great clinical relevance and social impactful. It
is associated to a variety of pathological events causing un altered excitability of peripheral nerves derived
by tissue damage depending on physical, biological and chemical injury. In the last years much
attention has been paid in the identification of novel molecules involved in mediating pain sensation
useful as therapeutic tools for the development of new analgesic drugs. Muscarinic receptors are
widely distributed both in the central and peripheral nervous system. It is known that muscarinic agonists
cause analgesic effects via spinal and supraspinal mechanisms. Considering that the analgesia induced
by cholinergic agonists is comparable to that observed with morphine, the identification of receptor subtypes involved
and the identification of the muscarinic ligands capable of selectively activate these receptors, is of considerable
interest for potential therapeutic application. In the present review we describe the role of muscarinic receptors in mediating
central and peripheral pain and the mechanisms downstream these receptors responsible of the modulation of nociceptive
stimuli. Moreover the therapeutic perspectives and the identification of potential drugs binding muscarinic receptors
involved in pain modulation will also be discussed.
Keywords: Acetylcholine, analgesia, bitopic ligands, muscarinic receptors, nociception, VR-1 channel.
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