Structure-activity relationship studies of sulfonylpiperazine analogues as novel negative allosteric modulators of human neuronal nicotinic receptors.
Structure-activity relationship studies of sulfonylpiperazine analogues as novel negative allosteric modulators of human neuronal nicotinic receptors.
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DOI：
10.1021/jm201294r
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发表时间：
2011-12-22
影响因子：
7.3
通讯作者：
McKay, Dennis B.
中科院分区：
文献类型：
--
作者：
Henderson, Brandon J.;Carper, Daniel J.;Gonzalez-Cestari, Tatiana F.;Yi, Bitna;Mahasenan, Kiran;Pavlovicz, Ryan E.;Dalefield, Martin L.;Coleman, Robert S.;Li, Chenglong;McKay, Dennis B.
神经元烟碱受体与几种疾病和病症有关，例如：自闭症、阿尔茨海默病、帕金森病、癫痫和各种形式的成瘾。为了了解尼古丁受体在这些疾病中的作用，拥有体外和体内靶向特定尼古丁受体的选择性分子将是有益的。我们的实验室先前已经鉴定了人α4β2（Hα4β2）和人α3β4（Hα3β4）烟碱受体的新型负变构调节剂。在以下研究中，研究了作为负变构调节剂的新型磺酰基哌嗪类似物对Hα4β2 nAChR和Hα3β4 nAChR的作用。这项工作，通过结构-活性关系（SAR）研究，描述了这些分子的化学特征，这是重要的效力和选择性对Hα4β2 nAChRs。
Neuronal nicotinic receptors have been implicated in several diseases and disorders such as: autism, Alzheimer’s disease, Parkinson’s disease, epilepsy, and various forms of addiction. To understand the role of nicotinic receptors in these conditions, it would be beneficial to have selective molecules that target specific nicotinic receptors in vitro and in vivo. Our laboratory has previously identified novel negative allosteric modulators of human α4β2 (Hα4β2) and human α3β4 (Hα3β4) nicotinic receptors. In the following studies, the effects of novel sulfonylpiperazine analogs that act as negative allosteric modulators on both Hα4β2 nAChRs and Hα3β4 nAChRs were investigated. This work, through structure-activity relationship (SAR) studies, describes the chemical features of these molecules that are important for both potency and selectivity on Hα4β2 nAChRs.
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影响因子：
3.6
作者：
McKay, Dennis B.;Chang, Cheng;Bergmeier, Stephen C.
通讯作者：
Bergmeier, Stephen C.
影响因子：
2.1
作者：
Carpino, LA;El-Faham, A
通讯作者：
El-Faham, A
影响因子：
56.9
作者：
Tapper, AR;McKinney, SL;Lester, HA
通讯作者：
Lester, HA
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影响因子：
33.6
作者：
Albuquerque EX;Pereira EF;Alkondon M;Rogers SW
通讯作者：
Rogers SW
影响因子：
4.7
作者：
Grady, Sharon R.;Drenan, Ryan M.;Marks, Michael J.
通讯作者：
Marks, Michael J.