5-(4-Hydroxy-6-methyl-2-oxo-2H-pyran-3-yl)-7-phenyl-2,3,6,7-tetrahydro-1,4-thiaze pines as compounds with high affinity at the benzodiazepine binding site on GABA(A) receptors.

Grunwald C; Kronbach C; Egerland U; Schindler R; Dieckmann R; Heinecke K; Hofgen N; Unverferth K

首页> 外文期刊>Die Pharmazie >5-(4-Hydroxy-6-methyl-2-oxo-2H-pyran-3-yl)-7-phenyl-2,3,6,7-tetrahydro-1,4-thiaze pines as compounds with high affinity at the benzodiazepine binding site on GABA(A) receptors.

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5-(4-Hydroxy-6-methyl-2-oxo-2H-pyran-3-yl)-7-phenyl-2,3,6,7-tetrahydro-1,4-thiaze pines as compounds with high affinity at the benzodiazepine binding site on GABA(A) receptors.

机译：5-（4-羟基-6-甲基-2-氧代-2H-吡喃-3-基）-7-苯基-2,3,6,7-四氢-1,4-噻嗪类化合物具有高亲和力GABA（A）受体上的苯二氮卓结合位点。

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A series of thiazepines has been studied as new ligands for the benzodiazepine binding site of the GABAA receptor. Compounds with high affinity and weak selectivity regarding alpha beta3gamma2, alpha2beta3gamma2, alpha3beta3gamma2, and alpha5beta3gamma2 subtypes were found. The pharmacophore is discussed based on experimental and theoretical results. The thiazepine sulfur atom was found to be able to act as hydrogen bond acceptor.

机译：已经研究了一系列噻嗪类作为GABAA受体的苯并二氮杂结合位点的新配体。发现了关于αbeta3gamma2，alpha2beta3gamma2，alpha3beta3gamma2和alpha5beta3gamma2亚型具有高亲和力和弱选择性的化合物。根据实验和理论结果讨论了药效基团。发现硫杂氮杂硫原子能够充当氢键受体。

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《Die Pharmazie》 |2011年第2期|共7页
作者
Grunwald C; Kronbach C; Egerland U; Schindler R; Dieckmann R; Heinecke K; Hofgen N; Unverferth K;
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1. 5-(4-Hydroxy-6-methyl-2-oxo-2H-pyran-3-yl)-7-phenyl-2,3,6,7-tetrahydro-1,4-thiaze pines as compounds with high affinity at the benzodiazepine binding site on GABA(A) receptors. [J] . Grunwald C, Kronbach C, Egerland U, Die Pharmazie . 2011,第2期

机译：5-（4-羟基-6-甲基-2-氧代-2H-吡喃-3-基）-7-苯基-2,3,6,7-四氢-1,4-噻嗪类化合物具有高亲和力GABA（A）受体上的苯二氮卓结合位点。
2. Comparison of in vivo and ex vivo (3H)flumazenil binding assays to determine occupancy at the benzodiazepine binding site of rat brain GABAA receptors. [J] . Li J, Fish RL, Cook SM, Neuropharmacology . 2006,第1期

机译：体内和离体（3H）氟马西尼结合测定法的比较，以确定在大鼠脑GABAA受体的苯二氮卓结合位点的占有率。
3. Triazoloquinazolinediones as novel high affinity ligands for the benzodiazepine site of GABA(A) receptors. [J] . Nilsson J, Gidlof R, Nielsen EO, Bioorganic and medicinal chemistry . 2011,第1期

机译：三唑并喹唑啉二酮是GABA（A）受体的苯二氮杂位的新型高亲和力配体。
4. Identification of ligand-receptor binding affinity using AlGaN/GaN high electron mobility transistors and binding-site models [C] . Wang Yu-Lin, Chih-Cheng Huang, You-Ren Hsu, IEEE International Conference on Nano/Micro Engineered and Molecular Systems . 2013

机译：使用AlGaN / GaN高电子迁移率晶体管和结合位点模型鉴定配体-受体结合亲和力
5. Topology characterization of a benzodiazepine-binding domain of GABA(A) receptor and anxiolytic-like effect of baicalin acting through the benzodiazepine-binding site. [D] . Xu, Zhiwen. 2005

机译：GABA（A）受体的苯并二氮杂-结合域的拓扑结构表征和黄ba苷通过苯并二氮杂binding结合位点的抗焦虑样作用。
6. Interaction of beta-carboline inverse agonists for the benzodiazepine site with another site on GABAA receptors. [O] . H K Im, W B Im, D B Carter, 1995

机译：β-咔啉反向激动剂对苯并二氮杂site位点与GABAA受体上另一个位点的相互作用。
7. Individually Monitoring Ligand-Induced Changes in the Structure of the GABAA Receptor at Benzodiazepine Binding Site and Non–Binding-Site Interfaces [O] . L. M. Sharkey, C. Czajkowski 2008

机译：单独监测配体诱导的苯并二氮杂结合位点和非结合位点界面GaBaa受体结构的变化

5-(4-Hydroxy-6-methyl-2-oxo-2H-pyran-3-yl)-7-phenyl-2,3,6,7-tetrahydro-1,4-thiaze pines as compounds with high affinity at the benzodiazepine binding site on GABA(A) receptors.

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