Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu 3) NAM probe (ML289) derived from a closely related mGlu 5 PAM

ShefflerD.J.; WenthurC.J.; BrunerJ.A.; CarringtonS.J.S.; VinsonP.N.; GogiK.K.; BlobaumA.L.; MorrisonR.D.; VamosM.; CosfordN.D.P.; StaufferS.R.; ScottDanielsJ.; NiswenderC.M.; JeffreyConnP.; LindsleyC.W.

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Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu 3) NAM probe (ML289) derived from a closely related mGlu 5 PAM

机译：开发一种新型的CNS - 渗透剂，代谢谷氨酸受体3（ML2）NAM探针（ML289）衍生自密切相关的MGLU 5 PAM

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Herein we report the discovery and SAR of a novel metabotropic glutamate receptor 3 (mGlu 3) NAM probe (ML289) with 15-fold selectivity versus mGlu 2. The mGlu 3 NAM was discovered via a 'molecular switch' from a closely related, potent mGlu 5 positive allosteric modulator (PAM), VU0092273. This NAM (VU0463597, ML289) displays an IC 50 value of 0.66 μM and is inactive against mGlu 5.

机译：在本文中，我们报告了一种新型代谢谷氨酸受体3（MGLU 3）NAM探针（ML289）的发现和SAR，其选择性为15倍。通过“分子开关”从密切相关，有效的“分子开关”发现了MGLU 3 NAM Mglu 5个正颠振调制器（PAM），VU0092273。该NAM（VU0463597，ML289）显示IC 50值为0.66μm，对MGLU 5无效。

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《Bioorganic and Medicinal Chemistry Letters》 |2012年第12期|共5页
作者
ShefflerD.J.; WenthurC.J.; BrunerJ.A.; CarringtonS.J.S.; VinsonP.N.; GogiK.K.; BlobaumA.L.; MorrisonR.D.; VamosM.; CosfordN.D.P.; StaufferS.R.; ScottDanielsJ.; NiswenderC.M.; JeffreyConnP.; LindsleyC.W.;
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Department of Pharmacology Vanderbilt University Medical Center Nashville TN 37232 United;

Department of Pharmacology Vanderbilt University Medical Center Nashville TN 37232 United;

Vanderbilt Center for Neuroscience Drug Discovery Vanderbilt University Medical Center Nashville;

Department of Pharmacology Vanderbilt University Medical Center Nashville TN 37232 United;

Department of Pharmacology Vanderbilt University Medical Center Nashville TN 37232 United;

Department of Pharmacology Vanderbilt University Medical Center Nashville TN 37232 United;

Department of Pharmacology Vanderbilt University Medical Center Nashville TN 37232 United;

Department of Pharmacology Vanderbilt University Medical Center Nashville TN 37232 United;

Apoptosis and Cell Death Research Program Conrad Prebys Center for Chemical Genomics Sanford;

Apoptosis and Cell Death Research Program Conrad Prebys Center for Chemical Genomics Sanford;

Department of Pharmacology Vanderbilt University Medical Center Nashville TN 37232 United;

Department of Pharmacology Vanderbilt University Medical Center Nashville TN 37232 United;

Department of Pharmacology Vanderbilt University Medical Center Nashville TN 37232 United;

Department of Pharmacology Vanderbilt University Medical Center Nashville TN 37232 United;

Department of Pharmacology Vanderbilt University Medical Center Nashville TN 37232 United;

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原文格式 PDF
正文语种 eng
中图分类药学;
关键词
Metabotropic glutamate receptor 3; mGlu 3; Molecular switch; NAM;

机译：代谢谷氨酸受体3;mglu 3;分子开关;nam;

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专利

1. Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu 3) NAM probe (ML289) derived from a closely related mGlu 5 PAM [J] . ShefflerD.J., WenthurC.J., BrunerJ.A., Bioorganic and Medicinal Chemistry Letters . 2012,第12期

机译：开发一种新型的CNS - 渗透剂，代谢谷氨酸受体3（ML2）NAM探针（ML289）衍生自密切相关的MGLU 5 PAM
2. Development of Novel, CNS Penetrant Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 1 (mGlu(1)), Based on an N-(3-Chloro-4-(1,3-dioxoisoindolin-2-yl)phenyl)-3-methylfuran-2-carboxamide Scaffold, That Potentiate Wild Type and Mutant mGlu(1) Receptors Found in Schizophrenics [J] . Garcia-Barrantes Pedro M., Cho Hyekyung P., Niswender Colleen M., Journal of Medicinal Chemistry . 2015,第20期

机译：基于N-（3-氯-4-（1,3-二氧代异吲哚-2-基）苯基）-3的新型代谢型谷氨酸受体亚型（mGlu（1））的中枢神经系统渗透性正变构调节剂的开发。 -甲基呋喃-2-羧酰胺支架，可增强精神分裂症患者的野生型和突变型mGlu（1）受体
3. Synthesis and SAR of a novel metabotropic glutamate receptor 4 (mGlu4) antagonist: unexpected 'molecular switch' from a closely related mGlu4 positive allosteric modulator. [J] . Utley T, Haddenham D, Salovich JM, Bioorganic and Medicinal Chemistry Letters . 2011,第23期

机译：新型代谢型谷氨酸受体4（mGlu4）拮抗剂的合成和SAR：与密切相关的mGlu4阳性变构调节剂产生的意外“分子转换”。
4. Digital Realization for Ca2+ Waves Stimulated by the (mGlu5) Receptors [C] . Mahsasadat Seyedbarhagh, Arash Ahmadi, Majid Ahmadi International Symposium on Signals, Circuits and Systems . 2021

机译：（MGLU5）受体刺激的CA2 +波的数字实现
5. Dopamine transporter (DAT), nicotinic acetylcholine receptor (nAChR), and metabotropic glutamate receptor 2 (mGlu2) irreversible probes for identifying anti-psychostimulant therapeutics. [D] . Aggarwal, Shaili. 2014

机译：多巴胺转运蛋白（DAT），烟碱乙酰胆碱受体（nAChR）和代谢型谷氨酸受体2（mGlu2）不可逆探针，用于鉴定抗精神兴奋药。
6. Development of a novel CNS-penetrant metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM [O] . Douglas J. Sheffler, Cody J. Wenthur, Joshua A. Bruner, -1

机译：衍生自密切相关的MGLU5 PAM的新型新型的CNS-渗透剂的新型CNS - 渗透剂代言谷氨酸受体3（ML289）
7. Probing the Metabotropic Glutamate Receptor 5 (mGlu5) Positive Allosteric Modulator (PAM) Binding Pocket: Discovery of Point Mutations That Engender a “Molecular Switch” in PAM Pharmacology [O] . Karen J. Gregory, Elizabeth D. Nguyen, Sean D. Reiff, 2013

机译：探测代谢谷氨酸受体5（MGLU5）阳性变构调节剂（PAM）结合口袋：发现PAM药理学中“分子开关”的点突变的发现

Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu 3) NAM probe (ML289) derived from a closely related mGlu 5 PAM

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