Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM.
about
Discovery of (R)-(2-fluoro-4-((-4-methoxyphenyl)ethynyl)phenyl) (3-hydroxypiperidin-1-yl)methanone (ML337), an mGlu3 selective and CNS penetrant negative allosteric modulator (NAM)Positive allosteric modulators of metabotropic glutamate 2 receptors in schizophrenia treatmentDrugs for allosteric sites on receptorsSubstituted 1-Phenyl-3-(pyridin-2-yl)urea negative allosteric modulators of mGlu5: discovery of a new tool compound VU0463841 with activity in rat models of cocaine addiction.2013 Philip S. Portoghese Medicinal Chemistry Lectureship: drug discovery targeting allosteric sites.Development of allosteric modulators of GPCRs for treatment of CNS disordersMolecular Insights into Metabotropic Glutamate Receptor Allosteric ModulationA novel metabotropic glutamate receptor 5 positive allosteric modulator acts at a unique site and confers stimulus bias to mGlu5 signalingDiscovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents.Design of 4-Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2.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.Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate ReceptorsIdentification of specific ligand-receptor interactions that govern binding and cooperativity of diverse modulators to a common metabotropic glutamate receptor 5 allosteric site.Allosteric modulation of Class C GPCRs: a novel approach for the treatment of CNS disorders.Progress toward advanced understanding of metabotropic glutamate receptors: structure, signaling and therapeutic indicationsFurther optimization of the mGlu5 PAM clinical candidate VU0409551/JNJ-46778212: Progress and challenges towards a back-up compoundDesign and Synthesis of N-Aryl Phenoxyethoxy Pyridinones as Highly Selective and CNS Penetrant mGlu3 NAMs.Design and Synthesis of mGlu2 NAMs with Improved Potency and CNS Penetration Based on a Truncated Picolinamide Core.
P2860
Q24625985-1B4EC886-E1C9-4EAD-B4E3-41E57B3CF114Q26852047-0CDC1D61-0778-47AA-B6B0-500F2FB74E11Q27006721-A3C6A58A-79F7-49EA-ADE7-3F62897BF669Q30432649-DE8BFB2A-52A2-493E-B563-51B7DCFC2691Q34243209-18DC87BF-A38E-4974-90C2-4E526E2376A6Q34373958-E680C6AA-0A27-4EAA-95D5-7E5762FD72C7Q34468639-FEF9E964-14C0-4F79-8E99-CBD29E28D454Q36717066-DAD34CED-A0CB-45BA-956C-0F7AAF998A50Q36733346-F1C2EBF9-75FF-4CFC-A69E-A1B5B612C568Q36755346-419AE661-CF58-4001-81A5-544AB9D19877Q36776760-5E72B830-8EEA-4733-855D-D07D36435B30Q37183072-4FA32931-1792-48D0-B023-A9837CECB85AQ37709393-9F590CBA-ECFD-4589-9693-312E751FE915Q38139547-23BA314A-D3C8-4DFA-BF28-8752177FFE2AQ38209092-3BDC6ECB-63AD-48B6-86EF-59C29C19F814Q41870911-7C407F3D-71FC-4237-A8C5-7ABD2C6F2963Q47758516-185A9E32-DBD4-4854-8808-6996B762054BQ47758525-72BB938E-240E-41E7-96B2-3BB18655D302
P2860
Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM.
description
2012 nî lūn-bûn
@nan
2012年の論文
@ja
2012年論文
@yue
2012年論文
@zh-hant
2012年論文
@zh-hk
2012年論文
@zh-mo
2012年論文
@zh-tw
2012年论文
@wuu
2012年论文
@zh
2012年论文
@zh-cn
name
Development of a novel, CNS-pe ...... m a closely related mGlu5 PAM.
@en
Development of a novel, CNS-pe ...... m a closely related mGlu5 PAM.
@nl
type
label
Development of a novel, CNS-pe ...... m a closely related mGlu5 PAM.
@en
Development of a novel, CNS-pe ...... m a closely related mGlu5 PAM.
@nl
prefLabel
Development of a novel, CNS-pe ...... m a closely related mGlu5 PAM.
@en
Development of a novel, CNS-pe ...... m a closely related mGlu5 PAM.
@nl
P2093
P2860
P50
P1476
Development of a novel, CNS-pe ...... om a closely related mGlu5 PAM
@en
P2093
Anna L Blobaum
Douglas J Sheffler
J Scott Daniels
Joshua A Bruner
Kiran K Gogi
Nicholas D P Cosford
Paige N Vinson
Ryan D Morrison
Shaun R Stauffer
Sheridan J S Carrington
P2860
P304
P356
10.1016/J.BMCL.2012.04.112
P407
P577
2012-04-30T00:00:00Z