Drug Discovery and Development Targeting NMDA Receptors

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (15 February 2024) | Viewed by 1717

Special Issue Editor


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Guest Editor
Philadelphia College of Pharmacy, St. Joseph’s University, Philadelphia, PA, USA
Interests: NMDA receptors; drug discovery; pharmaceutical profiling; drug targeting; Alzheimer’s disease
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Excitement in the NMDA receptor antagonist field was rekindled by the USA FDA approval of Memantine for the treatment of Alzheimer’s disease in 2003.  This special issue is a follow on of our special issue of a decade ago titled “NMDA Receptor Antagonists for the Treatment of CNS Disorders” in this journal.  As predicted then, there have been several positive developments in the field and thus a revised look is warranted.  An example is the approval of NMDAR antagonist ketamine for treatment resistant depression.  It represents a new mechanism for treatment of depression in over 3 decades.  Another antagonist, Dextromethorphan has been approved for depression.  Other NMDAR antagonists are being examined for treatment of pain.  While all glutamate receptors are possible drug targets, the NMDA receptor has been particularly attractive for many reasons, including feasibility and possible options of use.  The goal of this special issue is to examine progress in, current and future prospects in CNS drug discovery through this receptor.

Prof. Dr. Adeboye Adejare
Guest Editor

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Keywords

  • glutamate
  • NMDAR antagonist
  • CNS drug discovery
  • Depression
  • neuropathic pain
  • Ketamine
  • memory and learning
  • ionotropic receptors

Published Papers (1 paper)

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25 pages, 4716 KiB  
Review
GluN2A and GluN2B N-Methyl-D-Aspartate Receptor (NMDARs) Subunits: Their Roles and Therapeutic Antagonists in Neurological Diseases
by Amany Digal Ladagu, Funmilayo Eniola Olopade, Adeboye Adejare and James Olukayode Olopade
Pharmaceuticals 2023, 16(11), 1535; https://doi.org/10.3390/ph16111535 - 30 Oct 2023
Cited by 3 | Viewed by 1457
Abstract
N-methyl-D-aspartate receptors (NMDARs) are ion channels that respond to the neurotransmitter glutamate, playing a crucial role in the permeability of calcium ions and excitatory neurotransmission in the central nervous system (CNS). Composed of various subunits, NMDARs are predominantly formed by two [...] Read more.
N-methyl-D-aspartate receptors (NMDARs) are ion channels that respond to the neurotransmitter glutamate, playing a crucial role in the permeability of calcium ions and excitatory neurotransmission in the central nervous system (CNS). Composed of various subunits, NMDARs are predominantly formed by two obligatory GluN1 subunits (with eight splice variants) along with regulatory subunits GluN2 (GluN2A-2D) and GluN3 (GluN3A-B). They are widely distributed throughout the CNS and are involved in essential functions such as synaptic transmission, learning, memory, plasticity, and excitotoxicity. The presence of GluN2A and GluN2B subunits is particularly important for cognitive processes and has been strongly implicated in neurodegenerative diseases like Parkinson’s disease and Alzheimer’s disease. Understanding the roles of GluN2A and GluN2B NMDARs in neuropathologies provides valuable insights into the underlying causes and complexities of major nervous system disorders. This knowledge is vital for the development of selective antagonists targeting GluN2A and GluN2B subunits using pharmacological and molecular methods. Such antagonists represent a promising class of NMDA receptor inhibitors that have the potential to be developed into neuroprotective drugs with optimal therapeutic profiles. Full article
(This article belongs to the Special Issue Drug Discovery and Development Targeting NMDA Receptors)
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