ArticleACS chemical neuroscience2016
Discovery, Synthesis, and Preclinical Characterization of N-(3-Chloro-4-fluorophenyl)-1H-pyrazolo[4,3-b]pyridin-3-amine (VU0418506), a Novel Positive Allosteric Modulator of the Metabotropic Glutamate Receptor 4 (mGlu4).
Article in ACS chemical neuroscience, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 45 citations in OpenAlex.
- 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
- Targeting metabotropic glutamate receptors for symptomatic and disease-modifying treatment in Parkinson's disease.NPJ Parkinson's disease · 2025Review
- Update on mGlu4 modulator patents: 2017 to present.Expert opinion on therapeutic patents · 2025Review
- Elucidating the molecular logic of a metabotropic glutamate receptor heterodimer.Nature communications · 2024Article
- Advances and Insights in Positron Emission Tomography Tracers for Metabotropic Glutamate Receptor 4 Imaging.Journal of medicinal chemistry · 2024Review
- Mild and efficient synthesis and base-promoted rearrangement of novel isoxazolo[4,5-Beilstein journal of organic chemistry · 2024Article
- Straightforward and Efficient Protocol for the Synthesis of Pyrazolo [4,3-International journal of molecular sciences · 2023Article
- New 1,2,4-oxadiazole derivatives with positive mGluJournal of enzyme inhibition and medicinal chemistry · 2022Article
- Development and profiling of mGluBioorganic & medicinal chemistry letters · 2022Article
- Synthesis and Antiproliferative Activity of 2,4,6,7-Tetrasubstituted-2Molecules (Basel, Switzerland) · 2021Article
- Allosteric Molecular Switches in Metabotropic Glutamate Receptors.ChemMedChem · 2021Review
- Challenges in the Discovery and Optimization of mGluLetters in drug design & discovery · 2019Article
- SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic MBioorganic & medicinal chemistry letters · 2019Article
- Discovery of VU2957 (Valiglurax): An mGluACS medicinal chemistry letters · 2019Article
- Discovery of an Orally Bioavailable and Central Nervous System (CNS) Penetrant mGluJournal of medicinal chemistry · 2019Article
- Novel MBioorganic & medicinal chemistry letters · 2019Article
- Glutamatergic mechanisms in L-DOPA-induced dyskinesia and therapeutic implications.Journal of neural transmission (Vienna, Austria : 1996) · 2018Article
- Design and Synthesis ofACS medicinal chemistry letters · 2017Article
- Current Nondopaminergic Therapeutic Options for Motor Symptoms of Parkinson's Disease.Chinese medical journal · 2017Review
- Development and Antiparkinsonian Activity of VU0418506, a Selective Positive Allosteric Modulator of Metabotropic Glutamate Receptor 4 Homomers without Activity at mGlu2/4 Heteromers.ACS chemical neuroscience · 2016Article
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18 authors at 2 institutions in 1 country.
Funding
Abstract
The efficacy of positive allosteric modulators (PAMs) of the metabotropic glutamate receptor 4 (mGlu4) in preclinical rodent models of Parkinson's disease has been established by a number of groups. Here, we report an advanced preclinically characterized mGlu4 PAM, N-(3-chloro-4-fluorophenyl)-1H-pyrazolo[4,3-b]pyridin-3-amine (VU0418506). We detail the discovery of VU0418506 starting from a common picolinamide core scaffold and evaluation of a number of amide bioisosteres leading to the novel pyrazolo[4,3-b]pyridine head group. VU0418506 has been characterized as a potent and selective mGlu4 PAM with suitable in vivo pharmacokinetic properties in three preclinical safety species.
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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.