ArticleJournal of medicinal chemistry2013
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).
Article in Journal of medicinal chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 36 papers.
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Who cites it
36 citing papers in PubMed.
- Discovery of VU6066098: A Selective and CNS-Penetrant mGluACS chemical neuroscience · 2026Article
- Suppression of neuropathic pain hypersensitivity by TRPM8 is mediated by mGluR group II and III receptors acting differentially on distinct nociceptor inputs to spinal cord.Frontiers in pharmacology · 2026Article
- Development of a Peripherally Restricted 5-HTJACC. Basic to translational science · 2023Article
- Evaluation of the effects of the mGluPharmacological reports : PR · 2022Article
- Discovery of "Molecular Switches" within a Series of mGluACS bio & med chem Au · 2021Article
- Discovery of the First Selective MACS pharmacology & translational science · 2021Article
- Acetylenic Replacement of Albicidin's Methacrylamide Residue Circumvents Detrimental E/Z Photoisomerization and Preserves Antibacterial Activity.Chemistry (Weinheim an der Bergstrasse, Germany) · 2021Article
- The mGluJournal of neural transmission (Vienna, Austria : 1996) · 2020Article
- Presynaptic Release-regulating Metabotropic Glutamate Receptors: An Update.Current neuropharmacology · 2020Review
- Genetically Targeted Optical Control of an Endogenous G Protein-Coupled Receptor.Journal of the American Chemical Society · 2019Article
- VU0810464, a non-urea G protein-gated inwardly rectifying KBritish journal of pharmacology · 2019Article
- Drug metabolism in drug discovery and development.Acta pharmaceutica Sinica. B · 2018Review
- Discovery and Optimization of Potent and CNS Penetrant MACS chemical neuroscience · 2018Article
- Co-Activation of Metabotropic Glutamate Receptor 3 and Beta-Adrenergic Receptors Modulates Cyclic-AMP and Long-Term Potentiation, and Disrupts Memory Reconsolidation.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2017Article
- Immuno-pharmacological characterization of group II metabotropic glutamate receptors controlling glutamate exocytosis in mouse cortex and spinal cord.British journal of pharmacology · 2017Article
- Design and Synthesis of mGluACS medicinal chemistry letters · 2017Article
- Design and Synthesis ofACS medicinal chemistry letters · 2017Article
- Metabotropic glutamate receptor 2 inhibits thalamically-driven glutamate and dopamine release in the dorsal striatum.Neuropharmacology · 2017Article
- Recent advances in the medicinal chemistry of group II and group III mGlu receptors.MedChemComm · 2017Review
- Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate Receptors.Chemical reviews · 2016Review
Corrections and comments
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Authors and funding
10 authors.
Funding
Abstract
A multidimensional, iterative parallel synthesis effort identified a series of highly selective mGlu3 NAMs with submicromolar potency and good CNS penetration. Of these, ML337 resulted (mGlu3 IC50 = 593 nM, mGlu2 IC50 >30 μM) with B:P ratios of 0.92 (mouse) to 0.3 (rat). DMPK profiling and shallow SAR led to the incorporation of deuterium atoms to address a metabolic soft spot, which subsequently lowered both in vitro and in vivo clearance by >50%.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.