Abstract
This article describes recent medicinal chemistry progress toward selective potentiators of the metabotropic glutamate receptor 2 (mGluR2). Groups at Lilly and Merck have identified new classes of potentiators that exhibit selectivity for mGluR2 over the seven other subtypes of mGluRs. Structure-activity relationships as well as pharmacokinetic properties and in vivo activity are reviewed.
Keywords: glutamate, mglur, group II, potentiator, agonist
Current Topics in Medicinal Chemistry
Title: Positive Allosteric Modulators of the Metabotropic Glutamate Receptor Subtype 2 (mGluR2)
Volume: 5 Issue: 9
Author(s): Michael T. Rudd and John A. McCauley
Affiliation:
Keywords: glutamate, mglur, group II, potentiator, agonist
Abstract: This article describes recent medicinal chemistry progress toward selective potentiators of the metabotropic glutamate receptor 2 (mGluR2). Groups at Lilly and Merck have identified new classes of potentiators that exhibit selectivity for mGluR2 over the seven other subtypes of mGluRs. Structure-activity relationships as well as pharmacokinetic properties and in vivo activity are reviewed.
Export Options
About this article
Cite this article as:
Rudd T. Michael and McCauley A. John, Positive Allosteric Modulators of the Metabotropic Glutamate Receptor Subtype 2 (mGluR2), Current Topics in Medicinal Chemistry 2005; 5 (9) . https://dx.doi.org/10.2174/1568026054750281
DOI https://dx.doi.org/10.2174/1568026054750281 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Astrocyte-Neuron Interaction at Tripartite Synapses
Current Drug Targets Hydroxypyridinone Derivatives: A Fascinating Class of Chelators with Therapeutic Applications - An Update
Current Medicinal Chemistry PDZ Domain Protein-Protein Interactions: A Case Study with PICK1
Current Topics in Medicinal Chemistry The Structure and Functions of P-Glycoprotein
Current Medicinal Chemistry Cannabinoids and Sensory Neurones
Current Neuropharmacology Bioinformatic Screening of Autoimmune Disease Genes and Protein Structure Prediction with FAMS for Drug Discovery
Protein & Peptide Letters Neurovirulence of SARS CoV2: From Clinical Data to Preclinical Neuropsychological Exploration
Coronaviruses <i>Rhanterium suaveolens</i>, Vitamin E and C Pretreatment Prevents Valproic Acid Induced Renal Oxidant Damage
The Natural Products Journal Recent Patents and Discovery of Anti-inflammatory Agents from Marine Source
Recent Patents on Inflammation & Allergy Drug Discovery Alzheimer’s Disease and Autistic Spectrum Disorder: Is there any Association?
CNS & Neurological Disorders - Drug Targets Editorial [ Role of Ion Channels in Neurological Disorders Guest Editor: Johannes J. Krupp ]
CNS & Neurological Disorders - Drug Targets Investigation and Need of Bioequivalence Study: Methodology and Regulatory Requirement
Applied Clinical Research, Clinical Trials and Regulatory Affairs Role of the GABAA Receptor in Anxiety: Evidence from animal models, molecular and clinical psychopharmacology, and brain imaging studies
Current Neuropharmacology Bridging Over the Troubled Heterogeneity of SPG-Related Pathologies: Mechanisms Unite What Genetics Divide
Current Molecular Medicine Medicinal Chemistry and the Molecular Operating Environment (MOE): Application of QSAR and Molecular Docking to Drug Discovery
Current Topics in Medicinal Chemistry Blood Pressure Reduction in the Primary and Secondary Prevention of Stroke
Current Vascular Pharmacology Neuronal Ceroid Lipofuscinosis: The Increasing Spectrum of an Old Disease
Current Molecular Medicine Patents on Non-Viral Mediated Gene Delivery
Recent Patents on DNA & Gene Sequences A Retrospective Study on the Incidence of Seizures among Neurosurgical Patients Who Treated with Imipenem/Cilastatin or Meropenem
Current Pharmaceutical Biotechnology Update on the Evaluation and Management of Brief Resolved Unexplained Events (Previously Apparent Life-Threatening Events)
Reviews on Recent Clinical Trials