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
-
Stem Cell Therapy for Ischaemic Stroke: Translation from Preclinical Studies to Clinical Treatment
CNS & Neurological Disorders - Drug Targets EEG Correlates of Cognitive Functions and Neuropsychiatric Disorders: A Review of Oscillatory Activity and Neural Synchrony Abnormalities
Current Psychiatry Research and Reviews The Pathophysiological Basis of Carotid Baroreceptor Stimulation for the Treatment of Resistant Hypertension
Current Vascular Pharmacology Subject Index to Volume 4
Current Topics in Medicinal Chemistry Voltage-Gated Calcium Channels as Targets for the Treatment of Chronic Pain
Current Drug Targets - CNS & Neurological Disorders Modulation and Absorption of Xenobiotics: The Synergistic Role of CYP450 and P-gp Activities in Cancer and Neurodegenerative Disorders
Current Drug Metabolism Carbonic Anhydrase Inhibitors
Current Medicinal Chemistry - Immunology, Endocrine & Metabolic Agents C-terminus of Hsp70 Interacting Protein (CHIP) and Neurodegeneration: Lessons from the Bench and Bedside
Current Neuropharmacology Meet Our Editorial Board Member
CNS & Neurological Disorders - Drug Targets Metabolic Reprogramming of Human Cells in Response to Oxidative Stress: Implications in the Pathophysiology and Therapy of Mitochondrial Diseases
Current Pharmaceutical Design ABC Pumps and Their Role in Active Drug Transport
Current Topics in Medicinal Chemistry The Patch Clamp Technique in Ion Channel Research
Current Pharmaceutical Biotechnology Epileptogenicity and Epileptic Activity: Mechanisms in an Invertebrate Model Nervous System
Current Drug Targets Therapeutic Management of COVID-19 Patients: Clinical Manifestation and Limitations
Current Pharmaceutical Design Patent Selections :
Recent Patents on CNS Drug Discovery (Discontinued) Toward the Identification of Novel Carbonic Anhydrase XIV Inhibitors using 3D-QSAR Pharmacophore Model, Virtual Screening and Molecular Docking Study
Letters in Drug Design & Discovery Oxidative Damage Impact on Aging and Age-Related Diseases: Drug Targeting of Telomere Attrition and Dynamic Telomerase Activity Flirting with Imidazole-Containing Dipeptides
Recent Patents on Drug Delivery & Formulation Anti-Inflammatory Treatments for Chronic Diseases: A Review
Inflammation & Allergy - Drug Targets (Discontinued) Characterisation of a Neural Teratogenicity Assay Based on Human ESCs Differentiation Following Exposure to Valproic Acid
Current Medicinal Chemistry PET Radioligands for In Vivo Visualization of Neuroinflammation
Current Pharmaceutical Design