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Anticholinesterase induces nicotinic receptor modulation
Author(s) -
Sung JungJoon,
Kim Sang Jeong,
Lee Han Bo,
Chung JaeMyun,
Choi Yoo Mi,
Cha Choong Ik,
Suh YooHun,
Lee KwangWoo
Publication year - 1998
Publication title -
muscle and nerve
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.025
H-Index - 145
eISSN - 1097-4598
pISSN - 0148-639X
DOI - 10.1002/(sici)1097-4598(199809)21:9<1135::aid-mus4>3.0.co;2-8
Subject(s) - carbachol , chemistry , acetylcholinesterase , physostigmine , acetylcholine , muscarinic acetylcholine receptor , cholinergic , facilitation , acetylcholinesterase inhibitor , nicotinic agonist , desensitization (medicine) , cholinesterase , pharmacology , acetylcholine receptor , receptor , endocrinology , biochemistry , enzyme , neuroscience , biology
The effects of carbamate anticholinesterases, pyridostigmine and physostigmine, on the function of the nicotinic receptor (nAChR) in TE671 cells was studied, precluding their inhibition of acetylcholine hydrolysis by carbachol usage. In radioassay, the simultaneous application of carbachol and carbamates dose‐dependently decreased carbachol‐induced 22 Na + influx, compared with carbachol activation alone. Increasing cell preincubation in the presence of carbamates, however, potentiated influx at low concentrations in a time‐dependent manner. This facilitating effect of carbamates, even at high concentrations, was significantly increased by washing out these drugs and was blocked by pretreatment with diisopropylfluorophosphate. Similar results were also obtained in whole‐cell patch‐clamp study. There were insignificant changes in desensitization properties during facilitation. It is thus supposed that facilitation cannot be explained by the inhibition of acetylcholine hydrolysis. These results support a previous hypothesis that acetylcholinesterase might modulate nAChR by an unknown mechanism. In addition, the clinical effects of carbamates may be partly attributed to this facilitation. © 1998 John Wiley & Sons, Inc. Muscle Nerve 21: 1135–1144, 1998.