Nootropic alpha7 nicotinic receptor allosteric modulator derived from GABAA receptor modulators.

Ng HJ; Whittemore ER; Tran MBHogenkamp DJBroide RSJohnstone TBZheng LStevens KEGee KW

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Nootropic alpha7 nicotinic receptor allosteric modulator derived from GABAA receptor modulators.

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Activation of brain alpha7 nicotinic acetylcholine receptors (alpha7 nAChRs) has broad therapeutic potential in CNS diseases related to cognitive dysfunction, including Alzheimer's disease and schizophrenia. In contrast to direct agonist activation, positive allosteric modulation of alpha7 nAChRs would deliver the clinically validated benefits of allosterism to these indications. We have generated a selective alpha7 nAChR-positive allosteric modulator (PAM) from a library of GABAA receptor PAMs. Compound 6 (N-(4-chlorophenyl)-alpha-(4-chloro-phenyl)aminomethylene-3-methyl-5-isoxazol eacet-amide) evokes robust positive modulation of agonist-induced currents at alpha7 nAChRs, while preserving the rapid native characteristics of desensitization, and has little to no efficacy at other ligand-gated ion channels. In rodent models, it corrects sensory-gating deficits and improves working memory, effects consistent with cognitive enhancement. Compound 6 represents a chemotype for allosteric activation of alpha7 nAChRs, with therapeutic potential in CNS diseases with cognitive dysfunction.

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《Proceedings of the National Academy of Sciences of the United States of America》 |2007年第19期|8059-8064|共6页
作者
Ng HJ; Whittemore ER; Tran MBHogenkamp DJBroide RSJohnstone TBZheng LStevens KEGee KW;
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作者单位

Department of Pharmacology, School of Medicine, University of California, Irvine, CA 92697, USA.;

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收录信息美国《科学引文索引》(SCI);美国《生物学医学文摘》(MEDLINE);美国《化学文摘》(CA);
原文格式 PDF
正文语种英语
中图分类自然科学总论;
关键词
GABA Modulators; Nootropic Agents; Receptors; GABA-A; Nicotinic; GABA调节剂; 趋精神药类; 受体; 烟碱;

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机译：Modulation of the mammalian GABAA receptor by type I and type II positive allosteric modulators of the α7 nicotinic acetylcholine receptor
2. Functional characterization and high-throughput screening of positive allosteric modulators of alpha7 nicotinic acetylcholine receptors in IMR-32 neuroblastoma cells. [J] . Gopalakrishnan SM, Philip BM, Gronlien JHMalysz JAnderson DJGopalakrishnan MWarrior UBurns DJ Assay and drug development technologies . 2011,第6期

机译：Functional characterization and high-throughput screening of positive allosteric modulators of alpha7 nicotinic acetylcholine receptors in IMR-32 neuroblastoma cells.
3. Proximity-accelerated chemical coupling reaction in the benzodiazepine-binding site of gamma-aminobutyric acid type A receptors: superposition of different allosteric modulators. [J] . Tan KR, Gonthier A, Baur RErnst MGoeldner MSigel E The Journal of biological chemistry . 2007,第36期

机译：Proximity-accelerated chemical coupling reaction in the benzodiazepine-binding site of gamma-aminobutyric acid type A receptors: superposition of different allosteric modulators.
4. Localization of the GABAA receptor in the rat brain with a monoclonal antibody to the 57000 Mr peptide of the GABAA receptor/benzodiazepine receptor/Cl- channel complex [O] . AL de Blas, J Vitorica, P Friedrich 1988

机译：用针对GABAA受体/苯并二氮杂receptor受体/ Cl-通道复合物的57000 Mr肽的单克隆抗体将GABAA受体定位在大鼠脑中
5. Death receptor 5-mediated TNFR family signaling pathways modulate gamma-humulene-induced apoptosis in human colorectal cancer HT29 cells [O] . Lan, Y.H., Wu, Y.C., Wu, K.W., 2014

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6. Liposomer och Plana Lipidmembran med den Nikotinlika Acetylklinreceptorn (Liposomes and Planar Lipid Membranes with the Nicotinic Acetylcholine Receptor). [R] . Artursson, E. 2000

机译：Liposomer och plana Lipidmembran med den Nikotinlika acetylklinreceptorn（Liposomes and planar Lipid membranes with Nicotinic acetylcholine Receptor）。

Nootropic alpha7 nicotinic receptor allosteric modulator derived from GABAA receptor modulators.

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