Effect of organophosphorus insecticides on phosphorylation of the M(2) muscarinic acetylcholine receptor

IMR OpenIR

	Effect of organophosphorus insecticides on phosphorylation of the M(2) muscarinic acetylcholine receptor
其他题名	Effect of organophosphorus insecticides on phosphorylation of the M_2 muscarinic acetylcholine receptor
	Li Shuyin 1; Zou Liming 1; Pope Carry 2
	2008
发表期刊	NEURAL REGENERATION RESEARCH
ISSN	1673-5374
卷号	3 期号:4 页码:406-409
摘要	BACKGROUND: Organophosphorus insecticides may promote the accumulation of acetylcholine at synapses and the neuromuscular junction by inhibiting acetylcholinesterase activity to cause disturbance of neural signal conduction and induce a toxic reaction. Organophosphorus insecticides may act on M(2) muscarinic acetylcholine receptors, whose combination with G proteins is regulated by phosphorylation of G protein-coupled receptor kinase 2.
其他摘要	BACKGROUND: Organophosphorus insecticides may promote the accumulation of acetylcholine at synapses and the neuromuscular junction by inhibiting acetylcholinesterase activity to cause disturbance of neural signal conduction and induce a toxic reaction. Organophosphorus insecticides may act on M_2 muscarinic acetylcholine receptors, whose combination with G proteins is regulated by phosphorylation of G protein-coupled receptor kinase 2.OBJECTIVE: To investigate the effects of organophosphorus insecticides on the phosphorylation of G protein-coupled receptor kinase 2-mediated M_2 muscarinic acetylcholine receptors and to reveal other possible actions of organophosphorus insecticides.DESIGN, TIME AND SETTING: An observational study, which was performed in the Central Laboratory of Shenyang Medical College, and Department of Physiological Sciences, College of Veterinary Medicine, Oklahoma State University from June 2002 to December 2004.MATERIALS: Paraoxon, parathion, chlorpyrifos, and chlorpyrifos oxon were provided by Chem Service Company, USA, γ-P~(32) ATP and ~(35)SGTPγS by New England Nuclear Life Science Products, and recombinant β2-adrenergic receptor membrane protein by Sigma Company, USA.METHODS: The M_2 muscarinic acetylcholine receptor was extracted and purified from pig brain using affinity chromatography. Subsequently, the purified M_2 muscarinic acetylcholine receptor, G protein-coupled receptor kinase 2, and γ-P~(32) ATP were incubated with different concentrations of paraoxon and chlorpyrifos oxon together. The mixture then underwent polyacrylamide gel electrophoresis, and the gel film was dried and radioactively autographed to detect phosphorylation of the M_2 muscarinic acetylcholine receptor.Finally, the radio-labeled phosphorylated M_2 receptor protein band was excised for counting with an isotope liquid scintillation counter.MAIN OUTCOME MEASURES: Effects of chlorpyrifos oxon, paraoxon, chlorpyrifos, and parathion in different concentrations on the phosphorylation of the M_2 muscarinic acetylcholine receptor; effects of chlorpyrifos oxon on the phosphorylation of theβ-adrenergic receptor.RESULTS: Chlorpyrifos oxon could completely inhibit the phosphorylation of the M_2 muscarinic acetylcholine receptor, and its IC_(50) was 70 μmol/L. Chlorpyrifos could also inhibit the phosphorylation of the M_2 muscarinic acetylcholine receptor. However, paraoxon and parathion could not inhibit the phosphorylation of the M_2 muscarinic acetylcholine receptor. Chlorpyrifos oxon in different concentrations could also not inhibit the phosphorylation of the β2-adrenergic receptor catalyzed by G protein-coupled receptor kinase 2.CONCLUSION: Different kinds of organophosphorus insecticides have different effects on the phosphorylation of the G protein-coupled receptor kinase 2-mediated M_2 muscarinic acetylcholine receptor. Organophosphorus insecticides possibly have different toxic effects.
关键词	CHLORPYRIFOS-OXON IN-VITRO METHYL-PARAOXON RAT STRIATUM INHIBITION BINDING BRAIN DESENSITIZATION KINASE SEQUESTRATION organophosphorus insecticide antagonists G-protein-coupled receptor kinase 2 muscarinic acetylcholine receptor M(2) phosphorylation
收录类别	CSCD
语种	英语
CSCD记录号	CSCD:3299685
引用统计
文献类型	期刊论文
条目标识符	http://ir.imr.ac.cn/handle/321006/143607
专题	中国科学院金属研究所
作者单位	1.中国科学院金属研究所 2.华东师范大学
推荐引用方式 GB/T 7714	Li Shuyin,Zou Liming,Pope Carry. Effect of organophosphorus insecticides on phosphorylation of the M(2) muscarinic acetylcholine receptor[J]. NEURAL REGENERATION RESEARCH,2008,3(4):406-409.
APA	Li Shuyin,Zou Liming,&Pope Carry.(2008).Effect of organophosphorus insecticides on phosphorylation of the M(2) muscarinic acetylcholine receptor.NEURAL REGENERATION RESEARCH,3(4),406-409.
MLA	Li Shuyin,et al."Effect of organophosphorus insecticides on phosphorylation of the M(2) muscarinic acetylcholine receptor".NEURAL REGENERATION RESEARCH 3.4(2008):406-409.