The Recent Development of α7 Nicotinic Acetylcholine Receptor (nAChR) Ligands as Therapeutic Candidates for the Treatment of Central Nervous System (CNS) Diseases

被引：9

作者：

Beinat, Corinne ^{[1
]}

Banister, Samuel D. ^{[1
]}

Herrera, Marco ^{[2
]}

Kassiou, Michael ^{[3
,4
]}

机构：

[1] Stanford Univ, Sch Med, Dept Radiol, MIPS, Stanford, CA 94305 USA

[2] Stanford Univ, Sch Med, Dept Immunol, Stanford, CA 94305 USA

[3] Univ Sydney, Sch Chem, Sydney, NSW 2006, Australia

[4] Univ Sydney, Fac Hlth Sci, Sydney, NSW 2006, Australia

来源：

CURRENT PHARMACEUTICAL DESIGN | 2016年 / 22卷 / 14期

关键词：

Nicotinic receptors; schizophrenia; Alzheimer's disease; SEN12333; ALZHEIMERS-DISEASE; IN-VITRO; PARTIAL AGONIST; RAT-BRAIN; CONFORMATIONAL MIMICRY; MEDICINAL CHEMISTRY; COGNITIVE DEFICITS; AMIDE BOND; SCHIZOPHRENIA; BINDING;

D O I：

10.2174/1381612822666160127114125

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Homomeric alpha(7) nicotinic acetylcholine receptors (nAChRs) are implicated in the regulation of cognitive processes such as memory and attention and have potential as therapeutic targets for the treatment of the cognitive deficits associated with schizophrenia. Though numerous alpha(7) nAChR agonists have been developed, and several have progressed to clinical trials, these are derived from few common chemotypes. Consequently, many of these alpha(7) nAChR clinical candidates share unfavorable side-effect profile. SEN12333 represents a novel chemotype for the development of alpha(7) nAChR agonists, and exploration of this scaffold has produced structurally diverse ligands with promising pharmacological properties. This review will summarize structure-affinity and - activity relationships surrounding analogs of SEN12333.

引用

页码：2134 / 2151

页数：18

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