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Effects of aging on the interaction of quinuclidinyl benzilate, N-methylscopolamine, pirenzepine, and gallamine with brain muscarinic receptors.

作者信息

Surichamorn W, Kim O N, Lee N H, Lai W S, el-Fakahany E E

机构信息

Department of Pharmacology and Toxicology, School of Pharmacy, University of Maryland, Baltimore 21201.

出版信息

Neurochem Res. 1988 Dec;13(12):1183-91. doi: 10.1007/BF00971637.

DOI:10.1007/BF00971637
PMID:3237310
Abstract

The objective of the present study was to investigate the effects of senescence on the binding characteristics of muscarinic receptors by using [3H]quinuclidinyl benzilate ([3H]QNB) and [3H]N-methylscopolamine ([3H]NMS) as ligands in young (3 months), middle-age (10 months) and old (24 months) male Fischer 344 rats. Muscarinic receptor density was found to decrease significantly with aging in certain brain regions, depending on the ligand employed. Moreover, the relative proportions of M1 and M2 muscarinic receptor subtypes was not significantly altered by aging, except in the aged striatum. Furthermore, the dissociation kinetics of [3H]NMS in the cerebral cortex and their allosteric modulation by gallamine were only slightly influenced by age.

摘要

相似文献

1
Effects of aging on the interaction of quinuclidinyl benzilate, N-methylscopolamine, pirenzepine, and gallamine with brain muscarinic receptors.
Neurochem Res. 1988 Dec;13(12):1183-91. doi: 10.1007/BF00971637.
2
In vitro effects of gallamine on dissociation kinetics of (3H)N-methylscopolamine and (3H)pirenzepine from rat brain muscarinic receptors.
J Recept Res. 1986;6(1):47-61. doi: 10.3109/10799898609073923.
3
Gallamine binding to muscarinic M1 and M2 receptors, studied by inhibition of [3H]pirenzepine and [3H]quinuclidinylbenzilate binding to rat brain membranes.通过抑制[3H]哌仑西平和[3H]喹核醇基苯甲酸酯与大鼠脑膜的结合来研究加拉明与毒蕈碱M1和M2受体的结合。
Mol Pharmacol. 1986 Jul;30(1):58-68.
4
Multiple binding affinities of N-methylscopolamine to brain muscarinic acetylcholine receptors: differentiation from M1 and M2 receptor subtypes.N-甲基东莨菪碱与脑毒蕈碱型乙酰胆碱受体的多重结合亲和力:与M1和M2受体亚型的区分
J Pharmacol Exp Ther. 1986 Aug;238(2):554-63.
5
Regional distribution of M1, M2 and non-M1, non-M2 subtypes of muscarinic binding sites in rat brain.大鼠脑中毒蕈碱结合位点M1、M2以及非M1、非M2亚型的区域分布
J Pharmacol Exp Ther. 1990 Dec;255(3):1148-57.
6
On the interaction of gallamine with muscarinic receptor subtypes.
Eur J Pharmacol. 1990 Jul 3;182(2):335-45. doi: 10.1016/0014-2999(90)90292-e.
7
Allosteric regulation of cloned m1-m5 muscarinic receptor subtypes.克隆的毒蕈碱受体m1 - m5亚型的变构调节
Biochem Pharmacol. 1991 Oct 24;42(10):1927-32. doi: 10.1016/0006-2952(91)90591-r.
8
Quaternary forms of classical muscarinic antagonists distinguish subpopulations of muscarinic receptors: correlation with gallamine-defined subpopulations.经典毒蕈碱拮抗剂的季铵盐形式区分毒蕈碱受体亚群:与加拉明定义的亚群的相关性。
Biochem Biophys Res Commun. 1985 Feb 15;126(3):1242-50. doi: 10.1016/0006-291x(85)90319-5.
9
Gallamine exerts biphasic allosteric effects at muscarinic receptors.加拉明对毒蕈碱受体发挥双相变构效应。
Mol Pharmacol. 1989 Feb;35(2):173-6.
10
Influence of ligand choice on the apparent binding profile of gallamine to cardiac muscarinic receptors. Identification of three main types of gallamine-muscarinic receptor interactions.配体选择对加拉明与心脏毒蕈碱受体表观结合谱的影响。加拉明与毒蕈碱受体相互作用的三种主要类型的鉴定。
J Pharmacol Exp Ther. 1988 Sep;246(3):829-38.

引用本文的文献

1
Age-related alterations in pre-synaptic and receptor-mediated cholinergic functions in rat brain.大鼠脑中与年龄相关的突触前和受体介导的胆碱能功能改变。
Neurochem Res. 1998 May;23(5):719-26. doi: 10.1023/a:1022403308819.
2
Age-dependent decrease in the affinity of muscarinic M1 receptors in neocortex of rhesus monkeys.恒河猴新皮质中M1毒蕈碱受体亲和力的年龄依赖性降低。
Proc Natl Acad Sci U S A. 1991 Dec 15;88(24):11475-9. doi: 10.1073/pnas.88.24.11475.

本文引用的文献

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Protein measurement with the Folin phenol reagent.使用福林酚试剂进行蛋白质测定。
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Deficits in cholinergic enzymes and muscarinic receptors in the hippocampus and striatum of senescent rats: effect of chronic hydergine treatment.
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Comparison of [3H]pirenzepine and [3H]quinuclidinylbenzilate binding to muscarinic cholinergic receptors in rat brain.[3H]哌仑西平和[3H]喹核醇基苯甲酸酯与大鼠脑内毒蕈碱胆碱能受体结合的比较
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