N,N-Disubstituted piperazines and homopiperazines: Synthesis and affinities at alpha 4 beta 2*and alpha 7*neuronal nicotinic acetylcholine receptors
文献类型：期刊论文
| 作者 | Chen, Jianhong; Deaciuc, Agripina G.; Dwoskin, Linda P.; Crooks, Peter A.; Bai, Donglu
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| 刊名 | JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
 |
| 出版日期 | 2006-12 |
| 卷号 | 21期号:6页码:667-680 |
| 关键词 | piperazines homopiperazines neuronal nicotinic acetylcholine receptors alpha 4 beta 2 receptors |
| ISSN号 | 1475-6366 |
| DOI | 10.1080/14756360600900513 |
| 文献子类 | Article |
| 英文摘要 | A series of N, N-disubstituted piperazines and homopiperazines were prepared and evaluated for binding to natural alpha 4 beta 2(star) and alpha 7(star) neuronal nicotinic acetylcholine receptors (nAChRs) using whole brain membrane. Some compounds exhibited good selectivity for alpha 4 beta 2(star) nAChRs and did not interact with the alpha 7(star) nAChRs subtype. The most potent analogs were compounds 8-19 (K-i 10.4 mu M), 8-13 (K-i 12.0 mu M), and 8-24 (K-i 12.8 mM). Thus, linking together a pyridine pi-system and a cyclic amine moiety via a homopiperazine ring affords compounds with low affinity but with good selectivity for alpha 4 beta 2(star) nAChRs. |
| WOS关键词 | BETA-SUBUNITS ; EPIBATIDINE ANALOGS ; ANALGESIC ACTIVITY ; XENOPUS OOCYTES ; BINDING ; ANTAGONISTS ; SENSITIVITY ; ALPHA ; RAT ; AGONISTS |
| 资助项目 | NIDA NIH HHS[DA017548] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000242937500005 |
| 出版者 | TAYLOR & FRANCIS LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/273437]  |
| 专题 | 院士及顾问专家 |
| 通讯作者 | Crooks, Peter A. |
| 作者单位 | 1.Univ Kentucky, Coll Pharm, Dept Pharmaceut Sci, Lexington, KY 40536 USA 2.Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Chen, Jianhong,Deaciuc, Agripina G.,Dwoskin, Linda P.,et al. N,N-Disubstituted piperazines and homopiperazines: Synthesis and affinities at alpha 4 beta 2*and alpha 7*neuronal nicotinic acetylcholine receptors[J]. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY,2006,21(6):667-680. |
| APA | Chen, Jianhong,Deaciuc, Agripina G.,Dwoskin, Linda P.,Crooks, Peter A.,&Bai, Donglu.(2006).N,N-Disubstituted piperazines and homopiperazines: Synthesis and affinities at alpha 4 beta 2*and alpha 7*neuronal nicotinic acetylcholine receptors.JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY,21(6),667-680. |
| MLA | Chen, Jianhong,et al."N,N-Disubstituted piperazines and homopiperazines: Synthesis and affinities at alpha 4 beta 2*and alpha 7*neuronal nicotinic acetylcholine receptors".JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY 21.6(2006):667-680. |
入库方式： OAI收割
来源：上海药物研究所
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