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学科主题: 临床医学
题名:
Pharmacological characterization of [I-125]CHIBA-1006 binding, a new radioligand for alpha 7 nicotinic acetylcholine receptors, to rat brain membranes
作者: 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
发表日期: 2010-11-11
DOI: 10.1016/j.brainres.2010.08.095
卷: 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
所属项目编号: 06-46
项目资助者: National Institute of Biomedical Innovation of Japan
WOS记录号: WOS:000284252600012
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/54346
Appears in Collections:北京大学第一临床医学院_核医学科_期刊论文

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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

Recommended Citation:
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.
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