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Antinociception of intrathecal cholinesterase inhibitors and cholinergic receptors in rats
Author(s) -
Yoon M. H.,
Choi J. I.,
Jeong S. W.
Publication year - 2003
Publication title -
acta anaesthesiologica scandinavica
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.738
H-Index - 107
eISSN - 1399-6576
pISSN - 0001-5172
DOI - 10.1034/j.1399-6576.2003.00212.x
Subject(s) - physostigmine , neostigmine , edrophonium , pharmacology , muscarinic acetylcholine receptor , cholinesterase , nicotinic agonist , nociception , medicine , cholinergic , atropine , muscarinic acetylcholine receptor m2 , nicotinic antagonist , postsynaptic potential , acetylcholine receptor , acetylcholine , anesthesia , receptor , endocrinology
Background: Intrathecal cholinesterase inhibitors have been shown to have an antinociceptive effect which is mediated through the spinal cholinergic receptors, mainly muscarinic receptor. Spinal nicotinic receptor also has been involved in the control of nociception. Authors characterized the respective role of muscarinic or nicotinic receptor for the antinociception of cholinesterase inhibitors and further determined the antinociceptive potency of them. Methods: Rats were prepared with intrathecal catheters. Formalin‐induced flinching response was regarded as a nociceptive behavior. Results: Intrathecal neostigmine, physostigmine and edrophonium produced a dose‐dependent suppression of flinching in both phases. Atropine and the M 1 selective antagonist attenuated the effect of them, while the M 2 selective antagonist did not affect. M 3 , M 4 selective, and nicotinic receptor antagonists reversed the antinociception induced by edrophonium, but by neither neostigmine nor physostigmine. The ordering of potency was neostigmine > physostigmine > > edrophonium. Conclusion: These data indicate that the nicotinic receptor may be involved, at least in part, in the antinociceptive action of cholinesterase inhibitor at the spinal level, and M 1 receptor subtype may be a common pharmacologic site of action. Moreover, neostigmine is more potent than physostigmine and edrophonium.