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Brain regional acetylcholinesterase activity and muscarinic acetylcholine receptors in rats after repeated administration of cholinesterase inhibitors and its withdrawal.
Toxicol Appl Pharmacol. 2007 Mar; 219(2-3):151-61.TA

Abstract

Activity of acetylcholinesterase (AChE) and specific binding of [(3)H]quinuclidinyl benzilate (QNB), [(3)H]pirenzepine (PZP) and [(3)H]AF-DX 384 to muscarinic acetylcholine receptor (mAChR) preparations in the striatum, hippocampus and cortex of rats were determined 1, 6 and 11 days after the last treatment with an organophosphate DDVP, a carbamate propoxur or a muscarinic agonist oxotremorine as a reference for 7 and 14 days. AChE activity was markedly decreased in the three regions 1 day after the treatment with DDVP for 7 and 14 days with a gradual recovery 6 to 11 days, and much less decreased 1, 6 and 11 days after the treatment with propoxur for 7 days but not for 14 days in the hippocampus and cortex. The binding of [(3)H]-QNB, PZP and AF-DX 384 in the three regions was generally decreased by the treatment with DDVP for 7 and 14 days. Such down-regulations were generally restored 6 or 11 days after the treatment for 7 but not for 14 days. The down-regulation or up-regulation as measured by [(3)H]-QNB, PZP and AF-DX 384 was observed 1, 6 or 11 days after treatment with propoxur for 7 days and/or 14 days. Repeated treatment with oxotremorine produced similar effects except AChE activity to DDVP. These results suggest that repeated inhibition of AChE activity may usually cause down-regulation of mAChRs with some exception in the hippocampus when a reversible antiChE propoxur is injected.

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Authors+Show Affiliations

Kobayashi H
Department of Veterinary Medicine, Faculty of Agriculture, Iwate University, 3-18-8 Ueda, Morioka 020-8550, Japan. hk1664@iwate-u.ac.jp <hk1664@iwate-u.ac.jp>
Suzuki T
No affiliation info available
Sakamoto M
No affiliation info available
Hashimoto W
No affiliation info available
Kashiwada K
No affiliation info available
Sato I
No affiliation info available
Akahori F
No affiliation info available
Satoh T
No affiliation info available

MeSH

AcetylcholinesteraseAnimalsBrainCholinesterase InhibitorsDichlorvosLigandsMaleProtein BindingRatsRats, WistarReceptors, MuscarinicSubstance Withdrawal SyndromeTime Factors

Pub Type(s)

Journal Article

Language

eng

PubMed ID

17188317

Citation

Kobayashi, Haruo, et al. "Brain Regional Acetylcholinesterase Activity and Muscarinic Acetylcholine Receptors in Rats After Repeated Administration of Cholinesterase Inhibitors and Its Withdrawal." Toxicology and Applied Pharmacology, vol. 219, no. 2-3, 2007, pp. 151-61.
Kobayashi H, Suzuki T, Sakamoto M, et al. Brain regional acetylcholinesterase activity and muscarinic acetylcholine receptors in rats after repeated administration of cholinesterase inhibitors and its withdrawal. Toxicol Appl Pharmacol. 2007;219(2-3):151-61.
Kobayashi, H., Suzuki, T., Sakamoto, M., Hashimoto, W., Kashiwada, K., Sato, I., Akahori, F., & Satoh, T. (2007). Brain regional acetylcholinesterase activity and muscarinic acetylcholine receptors in rats after repeated administration of cholinesterase inhibitors and its withdrawal. Toxicology and Applied Pharmacology, 219(2-3), 151-61.
Kobayashi H, et al. Brain Regional Acetylcholinesterase Activity and Muscarinic Acetylcholine Receptors in Rats After Repeated Administration of Cholinesterase Inhibitors and Its Withdrawal. Toxicol Appl Pharmacol. 2007;219(2-3):151-61. PubMed PMID: 17188317.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Brain regional acetylcholinesterase activity and muscarinic acetylcholine receptors in rats after repeated administration of cholinesterase inhibitors and its withdrawal. AU - Kobayashi,Haruo, AU - Suzuki,Tadahiko, AU - Sakamoto,Maki, AU - Hashimoto,Wataru, AU - Kashiwada,Keiko, AU - Sato,Itaru, AU - Akahori,Fumiaki, AU - Satoh,Tetsuo, Y1 - 2006/11/11/ PY - 2006/08/31/received PY - 2006/11/04/revised PY - 2006/11/06/accepted PY - 2006/12/26/pubmed PY - 2007/3/30/medline PY - 2006/12/26/entrez SP - 151 EP - 61 JF - Toxicology and applied pharmacology JO - Toxicol Appl Pharmacol VL - 219 IS - 2-3 N2 - Activity of acetylcholinesterase (AChE) and specific binding of [(3)H]quinuclidinyl benzilate (QNB), [(3)H]pirenzepine (PZP) and [(3)H]AF-DX 384 to muscarinic acetylcholine receptor (mAChR) preparations in the striatum, hippocampus and cortex of rats were determined 1, 6 and 11 days after the last treatment with an organophosphate DDVP, a carbamate propoxur or a muscarinic agonist oxotremorine as a reference for 7 and 14 days. AChE activity was markedly decreased in the three regions 1 day after the treatment with DDVP for 7 and 14 days with a gradual recovery 6 to 11 days, and much less decreased 1, 6 and 11 days after the treatment with propoxur for 7 days but not for 14 days in the hippocampus and cortex. The binding of [(3)H]-QNB, PZP and AF-DX 384 in the three regions was generally decreased by the treatment with DDVP for 7 and 14 days. Such down-regulations were generally restored 6 or 11 days after the treatment for 7 but not for 14 days. The down-regulation or up-regulation as measured by [(3)H]-QNB, PZP and AF-DX 384 was observed 1, 6 or 11 days after treatment with propoxur for 7 days and/or 14 days. Repeated treatment with oxotremorine produced similar effects except AChE activity to DDVP. These results suggest that repeated inhibition of AChE activity may usually cause down-regulation of mAChRs with some exception in the hippocampus when a reversible antiChE propoxur is injected. SN - 0041-008X UR - https://www.unboundmedicine.com/medline/citation/17188317/Brain_regional_acetylcholinesterase_activity_and_muscarinic_acetylcholine_receptors_in_rats_after_repeated_administration_of_cholinesterase_inhibitors_and_its_withdrawal_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0041-008X(06)00420-0 DB - PRIME DP - Unbound Medicine ER -