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Pharmacological characterization of [I-125]CHIBA-1006 binding, a new radioligand for alpha 7 nicotinic acetylcholine receptors, to rat brain membranes
Wu, Jin1; Toyohara, Jun1; Tanibuchi, Yuko1; Fujita, Yuko1; Zhang, Jichun1; Chen, Hongxian1; Matsuo, Masaaki2; Wang, Rong Fu3; Hashimoto, Kenji1
关键词Nicotinic Receptor Receptor Binding Assay Brain Rat
刊名BRAIN RESEARCH
2010-11-11
DOI10.1016/j.brainres.2010.08.095
1360页:130-137
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Neurosciences
研究领域[WOS]Neurosciences & Neurology
关键词[WOS]POSITRON-EMISSION-TOMOGRAPHY ; COGNITIVE DEFICITS ; AGONIST SSR180711 ; DRUG DISCOVERY ; MOUSE-BRAIN ; BUNGAROTOXIN ; SCHIZOPHRENIA ; LOCALIZATION ; SUBTYPES ; TARGETS
英文摘要

The alpha 7 nicotinic acetylcholine receptors (nAChRs) play an important role in the pathophysiology of neuropsychiatric diseases such as schizophrenia and Alzheimer′s disease. However, there are currently no suitable small molecule radioligands for imaging alpha 7 nAChRs in the brain. In this study, we synthesized the novel radioligand [I-125]4-iodophenyl 1,4-diazaicyclo[3.2.2]nonane-4-carboxylate ([I-125]CHIBA-1006), a iodine-derivative of the selective alpha 7 nAChR agonist SSR180711, and studied the characterization of [I-125]CHIBA-1006 binding to rat brain membranes. The assays of [I-125]CHIBA-1006 binding to rat brain membranes were performed at 4 degrees C. The presence of a single saturable high-affinity binding component for [I-125] CHIBA-1006 in the rat brain was shown. Scatchard analysis revealed an apparent equilibrium dissociation constant (K-d) of 88.2 +/- 21.4 nM and a maximal number of binding sites (B-max) of 65.4 +/- 6.8 fmol/mg protein (mean +/- SEM, n=4). The specific binding of [I-125]CHIBA-1006 was inhibited by a number of alpha 7 nAChR-selective ligands (e.g., unlabeled CHIBA-1006, SSR180711, CHIBA-1001, MG624 and A844606), suggesting a similarity among 7 nAChR pharmacological profiles. In contrast, alpha-bungarotoxin, MLA, and nicotine showed very weak affinity for [I-125]CHIBA-1006 binding. The regional distribution of [I-125]CHIBA-1006 binding to crude membranes from dissected regions of the rat brain was different from that of [I-125] alpha-bungarotoxin binding, suggesting that [I-125]CHIBA-1006 binding sites may not be identical to [I-125]alpha-bungarotoxin binding sites in the rat brain. The present findings suggest that [I-125]CHIBA-1006 would be a useful new small molecule radioligand for alpha 7 nAChRs in the brain. (C) 2010 Elsevier B.V. All rights reserved.

语种英语
WOS记录号WOS:000284252600012
项目编号06-46
资助机构National Institute of Biomedical Innovation of Japan
引用统计
被引频次:7[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/54346
专题北京大学第一临床医学院_核医学科
作者单位1.Nard Inst Ltd, Amagasaki, Hyogo 6600805, Japan
2.Chiba Univ, Ctr Forens Mental Hlth, Div Clin Neurosci, Chiba 2608670, Japan
3.Peking Univ, Hosp 1, Dept Nucl Med, Beijing 100034, Peoples R China
推荐引用方式
GB/T 7714
Wu, Jin,Toyohara, Jun,Tanibuchi, Yuko,et al. Pharmacological characterization of [I-125]CHIBA-1006 binding, a new radioligand for alpha 7 nicotinic acetylcholine receptors, to rat brain membranes[J]. BRAIN RESEARCH,2010,1360:130-137.
APA Wu, Jin.,Toyohara, Jun.,Tanibuchi, Yuko.,Fujita, Yuko.,Zhang, Jichun.,...&Hashimoto, Kenji.(2010).Pharmacological characterization of [I-125]CHIBA-1006 binding, a new radioligand for alpha 7 nicotinic acetylcholine receptors, to rat brain membranes.BRAIN RESEARCH,1360,130-137.
MLA Wu, Jin,et al."Pharmacological characterization of [I-125]CHIBA-1006 binding, a new radioligand for alpha 7 nicotinic acetylcholine receptors, to rat brain membranes".BRAIN RESEARCH 1360(2010):130-137.
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