Discovery of novel conformationally constrained tropane-based biaryl and arylacetylene ligands as potent and selective norepinephrine transporter inhibitors and potential antidepressants.
Discovery of novel conformationally constrained tropane-based biaryl and arylacetylene ligands as potent and selective norepinephrine transporter inhibitors and potential antidepressants.
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发现新型构象受限的托烷基联芳基和芳基乙炔配体作为有效和选择性去甲肾上腺素转运蛋白抑制剂和潜在的抗抑郁药。
DOI：
10.1016/j.bmcl.2005.03.083
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发表时间：
2005
期刊：
影响因子：
--
通讯作者：
Kozikowski,AlanP
中科院分区：
文献类型：
--
作者：
Zhou,Jia;Klass,Thomas;Johnson,KennethM;Giberson,KellyM;Kozikowski,AlanP
To further explore the structure–activity relationships of conformationally constrained tropanes, a number of new biaryl and arylacetylene analogs were designed and synthesized. Some of these compounds such as 3a–b, 3d, 3f–h, 5b, and 7g were found to be highly potent and selective or mixed norepinephrine transporter (NET) inhibitors with Kivalues of 0.8–9.4nM. Moreover, all of these compounds display weak to extremely weak muscarinic receptor binding affinity, indicating that as potential antidepressants, they may overcome certain side effects that are of concern with other antidepressants, which are thought to be mediated by their anticholinergic properties.
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影响因子：
10.4
作者：
Lupolt SN;Santo RE;Kim BF;Green C;Codling E;Rule AM;Chen R;Scheckel KG;Strauss M;Cocke A;Little NG;Rupp VC;Viqueira R;Illuminati J;Epp Schmidt A;Nachman KE
通讯作者：
Nachman KE
去甲肾上腺素（去甲肾上腺素）和抑郁症
影响因子：
6
作者：
M. Moffaert;M. Dierick
通讯作者：
M. Dierick
(Z)-9-(杂芳基亚甲基)-7-氮杂三环[4.3.1.0(3,7)]癸烷的合成和药理学评价：噻吩类似物作为有效的去甲肾上腺素转运蛋白抑制剂。
影响因子：
2.7
作者：
Zhou,Jia;Kläss,Thomas;Zhang,Ao;Johnson,KennethM;Wang,ChengZ;Ye,Yanping;Kozikowski,AlanP
通讯作者：
Kozikowski,AlanP
基于哌啶的诺卡因/莫达非尼混合配体作为高效单胺转运蛋白抑制剂：通过合理的先导杂交实现有效的药物发现。
影响因子：
7.3
作者：
Zhou,Jia;He,Rong;Johnson,KennethM;Ye,Yanping;Kozikowski,AlanP
通讯作者：
Kozikowski,AlanP
苯并噻吩氧基苯丙胺，新型血清素和去甲肾上腺素再摄取双重抑制剂。
影响因子：
2.7
作者：
John R. Boot;G. Brace;C. Delatour;Nancy Dezutter;John Fairhurst;J. Findlay;Peter Thaddeus Gallagher;I. Hoes;S. Mahadevan;S. N. Mitchell;Richard E. Rathmell;Simon James Richards;R. G. Simmonds;Louise Wallace;M. Whatton
通讯作者：
M. Whatton