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Recent progress on the identification of metabotropic glutamate 4 receptor ligands and their potential utility as CNS therapeutics.近期代谢型谷氨酸 4 受体配体鉴定的进展及其作为中枢神经系统治疗药物的潜在应用。
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2
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3
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Recent advances in the drug discovery of metabotropic glutamate receptor 4 (mGluR4) activators for the treatment of CNS and non-CNS disorders.代谢型谷氨酸受体 4（mGluR4）激动剂在中枢神经系统和非中枢神经系统疾病治疗药物研发方面的最新进展。
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本文引用的文献

1
Tricyclic thiazolopyrazole derivatives as metabotropic glutamate receptor 4 positive allosteric modulators.三环噻唑并吡唑衍生物作为代谢型谷氨酸受体 4 的正变构调节剂。
J Med Chem. 2011 Jul 28;54(14):5070-81. doi: 10.1021/jm200290z. Epub 2011 Jul 1.
2
Solution-phase parallel synthesis and SAR of homopiperazinyl analogs as positive allosteric modulators of mGlu₄.溶液相平行合成及同哌嗪基类似物作为 mGlu₄ 正变构调节剂的 SAR 研究。
ACS Comb Sci. 2011 Mar 14;13(2):159-65. doi: 10.1021/co1000508. Epub 2011 Feb 21.
3
Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu(4)) with CNS exposure in rats.发现、合成和结构活性关系研究一系列 N-(4-乙酰氨基)苯吡啶甲酰胺作为代谢型谷氨酸受体 4（mGlu(4)）的正别构调节剂，在大鼠中枢神经系统中具有暴露量。
J Med Chem. 2011 Feb 24;54(4):1106-10. doi: 10.1021/jm101271s. Epub 2011 Jan 19.
4
Integrated synthetic, pharmacological, and computational investigation of cis-2-(3,5-dichlorophenylcarbamoyl)cyclohexanecarboxylic acid enantiomers as positive allosteric modulators of metabotropic glutamate receptor subtype 4.顺式-2-(3,5-二氯苯甲酰胺基)环己烷羧酸对映异构体作为代谢型谷氨酸受体亚型 4 的正别构调节剂的综合合成、药理学和计算研究。
ChemMedChem. 2011 Jan 3;6(1):131-40. doi: 10.1002/cmdc.201000378.
5
Orthosteric- and allosteric-induced ligand-directed trafficking at GPCRs.G蛋白偶联受体上的正构和变构诱导配体导向的转运
Curr Opin Drug Discov Devel. 2010 Sep;13(5):587-94.
6
Metabotropic glutamate receptor 4 novel agonist LSP1-2111 with anxiolytic, but not antidepressant-like activity, mediated by serotonergic and GABAergic systems.代谢型谷氨酸受体 4 新型激动剂 LSP1-2111 通过 5-羟色胺能和 GABA 能系统具有抗焦虑作用，但没有抗抑郁样作用。
Neuropharmacology. 2010 Dec;59(7-8):627-34. doi: 10.1016/j.neuropharm.2010.08.008. Epub 2010 Aug 14.
7
Exploration of structure-based drug design opportunities for mGluRs.基于结构的代谢型谷氨酸受体药物设计机会的探索。
Neuropharmacology. 2011 Jan;60(1):93-101. doi: 10.1016/j.neuropharm.2010.08.001. Epub 2010 Aug 10.
8
Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS).通过功能高通量筛选（HTS）鉴定的新型 4-（苯磺酰胺基）苯基乙酰胺 mGlu4 正变构调节剂（PAMs）的合成和 SAR。
Bioorg Med Chem Lett. 2010 Sep 1;20(17):5175-8. doi: 10.1016/j.bmcl.2010.07.007. Epub 2010 Jul 8.
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Potential psychiatric applications of metabotropic glutamate receptor agonists and antagonists.代谢型谷氨酸受体激动剂和拮抗剂的潜在精神科应用。
CNS Drugs. 2010 Aug;24(8):669-93. doi: 10.2165/11533230-000000000-00000.
10
An orally bioavailable positive allosteric modulator of the mGlu4 receptor with efficacy in an animal model of motor dysfunction.一种具有口服生物利用度的 mGlu4 受体正变构调节剂，在运动功能障碍动物模型中具有疗效。
Bioorg Med Chem Lett. 2010 Aug 15;20(16):4901-5. doi: 10.1016/j.bmcl.2010.06.078. Epub 2010 Jun 25.

近期代谢型谷氨酸 4 受体配体鉴定的进展及其作为中枢神经系统治疗药物的潜在应用。

Recent progress on the identification of metabotropic glutamate 4 receptor ligands and their potential utility as CNS therapeutics.

机构信息

Chemical & Pharmacokinetic Sciences, Lundbeck Research USA, 215 College Road, Paramus, New Jersey 07652, USA.

出版信息

ACS Chem Neurosci. 2011 Aug 17;2(8):433-49. doi: 10.1021/cn200043e. Epub 2011 Jun 14.

DOI:10.1021/cn200043e
PMID:22860170
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3369748/
Abstract

This Review describes recent activity in the advancement of ligands for the metabotropic glutamate 4 receptor subtype and their potential utility as central nervous system (CNS) therapeutics. Until recently, there was a paucity of compounds with suitable selectivity and druglike properties to elucidate the value of this target. The search for selective entities has led several groups to the investigation of allosteric modulators as a path to optimization of potential ligands. Recent efforts, discussed here, have afforded a variety of derivatives with improvements in potency, solubility, and pharmacokinetic properties that garner support for continued investigation and optimization.

摘要

本综述描述了最近在推进代谢型谷氨酸 4 受体亚型配体方面的进展，以及它们作为中枢神经系统 (CNS) 治疗药物的潜在用途。直到最近，具有适当选择性和类药性的化合物还很少，无法阐明该靶点的价值。对选择性实体的研究促使一些研究小组开始研究变构调节剂，以优化潜在配体。本文讨论了最近的研究进展，这些研究进展提供了各种具有更高活性、更好水溶性和更佳药代动力学性质的衍生物，为进一步研究和优化提供了支持。