N‐Methyl‐D‐aspartate Antagonists and Neuropathic Pain: The Search for Relief.

Childers, Wayne E.; Baudy, Reinhardt B

doi:10.1002/chin.200731184

Cited by 24 publications

(53 citation statements)

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“…5,48 The cloning of NMDA receptor subunits triggered a subsequent campaign to identify receptor subtypeselective compounds. The dissection of subunit-selective NMDA receptor functions will promote understanding of the molecular mechanisms underlying physiological and pathological processes, and the development of NMDA receptor subunit-selective antagonists has been the subject of intense research in recent years.…”

Section: Pharmacology: Nr2a Vs Nr2b Receptor Antagonistmentioning

confidence: 99%

“…83 Indeed, NR2B antagonists, such as ifenprodil and related compounds, are effective in neuropathic pain in animals and in patients, and show better separation between efficacy and adverse effects than nonselective NMDA receptor blockers. 5,49 For example, antinociceptive doses of ifenprodil and eliprodil appear to be devoid of psychotomimetic effects, as well as of motor deficits. Importantly, these drugs do not lead to abuse and may otherwise have effect on the development of morphine-induced conditioned place preference.…”

Section: Preclinical and Clinical Studies Of Nmda Receptor Antagonistsmentioning

confidence: 99%

“…84,85 After the identification of ifenprodil, a second generation of compounds was developed, such as Ro 25-6981 and CI-1041, which have demonstrated efficacy in a number of animal pain models, apparently with superior adverse effect profiles, relative to earlier analogues. 5,77 One compound, traxoprodil (CP-101,606) has progressed to phase II clinical trials. A preliminary report indicates that intravenous administration of the compound is effective in patients suffering from central pain such as spinal cord injury, but show no typical psychotomimetic effects.…”

Section: Preclinical and Clinical Studies Of Nmda Receptor Antagonistsmentioning

confidence: 99%

“…A preliminary report indicates that intravenous administration of the compound is effective in patients suffering from central pain such as spinal cord injury, but show no typical psychotomimetic effects. 5 Therefore, although there is debate on spinal versus brain NR2B in mediating antinociceptive effects, NR2B-containing NMDA receptor is one of the best potential targets for neuropathic pain. …”

Section: Preclinical and Clinical Studies Of Nmda Receptor Antagonistsmentioning

confidence: 99%

“…Among several candidates, the NMDA receptor, one of the major glutamate receptors that is important for synaptic plasticity, has been intensively investigated by both academic and pharmaceutical companies. [3][4][5][6] The aim of this review is to address recent progress in studying NMDA receptors in neuropathic pain. We first review the basic properties of the NMDA receptor and its role in synaptic plasticity, and then review NMDA receptor-dependent plasticity at different levels of pain transmission, from spinal cord to anterior cingulate cortex (ACC).…”

Section: Introductionmentioning

confidence: 99%

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Targeting the NMDA Receptor Subunit NR2B for the Treatment of Neuropathic Pain

2009

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Summary:Neuropathic pain is generally defined as a chronic pain state resulting from peripheral or central nerve injury, or both. An effective treatment for neuropathic pain is still lacking. The NMDA receptor, one type of the ionotropic glutamate receptors, is known to be important for triggering long-lasting changes in synapses. NMDA receptor-dependent synaptic plasticity plays roles not only in physiological functions such as learning and memory, but also in unwanted pathological conditions such as chronic pain. This review addresses recent progress on NMDA receptors in neuropathic pain, with particular emphasis on the NR2B-subunitcontaining receptors. The expression and function of NMDA receptors in synaptic plasticity in the pain transmission pathway from dorsal root ganglia to the anterior cingulate cortex is reviewed, and preclinical and clinical investigations of selective NMDA receptor in neuropathic pain are discussed. The NMDA receptors, in particular NR2B-containing NMDA receptors, serve as promising targets for treatment of neuropathic pain.

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Section: Pharmacology: Nr2a Vs Nr2b Receptor Antagonistmentioning

confidence: 99%

Section: Preclinical and Clinical Studies Of Nmda Receptor Antagonistsmentioning

confidence: 99%

Section: Preclinical and Clinical Studies Of Nmda Receptor Antagonistsmentioning

confidence: 99%

Section: Preclinical and Clinical Studies Of Nmda Receptor Antagonistsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Targeting the NMDA Receptor Subunit NR2B for the Treatment of Neuropathic Pain

2009

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Colorimetric chiral fluorescent sensors for Eu³⁺ and sequential enantioselective sensing of malate anion

Liu

Wang

et al. 2018

Chirality

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Novel phenanthroline Schiff base fluorescent sensors L1, L2, and D1 were designed and synthesized. The sensing abilities of the compounds in the presence of metal cations (Li , Na , K , Ag , Mg , Ba , Ca , Mn , Pb , Hg , Ni , Zn , Cd , Co , Cu , Cr , Fe , Fe , Al , and Eu ) were studied by UV-vis and fluorescent spectroscopy. The compounds L1, L2, and D1 could act as Eu ion turn-off fluorescent sensors based on ligand-to-metal binding mechanism in DMSO-H O solution (v/v = 1:1, 10 mM Tris, pH = 7.4). Additionally, the L1-Eu and D1-Eu complexes could be applied as turn-on enantioselective sensors sensing of malate anion isomers with color changes. Furthermore, biological experiments using living PC-12 cells demonstrated that L1 and D1 had excellent membrane permeability and could be used as effective fluorescent sensors for detecting Eu and malate anion in living cells.

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2020 foresight: Envisioning therapeutic innovations for pain

Hamza

Dionne

2009

Drug Discovery Today: Therapeutic Strategies

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"Pain is a gift" is an adage frequently told to medical students to imply the important protective role of pain sensation against tissue injury. However, when pain persists and turns from a warning signal to a continually annoying or distressing symptom, it can hardly be called a gift. Chronic pain results in continual suffering in millions of patients and affects their work performance and quality of life with a large socioeconomic impact on the patient and the community [1].The magnitude and consequences of pain cannot usually be ignored. Ever since the early civilizations when bark and leaves of the willow were used to treat painful conditions, clinicians have sought to put an end to people's suffering. Yet a satisfactory cure for chronic pain, particularly that of neuropathic origin or consequent to bone metastasis, has not been achieved. As reviewed previously [2], there are several reasons contributing to this failure, including the limitation of the present animal and experimental clinical models of pain to identify novel analgesics other than those with mechanisms similar to the drug class that they were originally designed to test. Most of the present models were primarily designed to study molecules targeting a narrow scope of pain targets, which make them unsuitable to screen new investigational drugs targeting newly recognized or the still unidentified wide array of mediators and molecular-genetic modulators of pain. We review here emerging new approaches to analgesic development that promise to translate molecular-genetic findings of the past decade into new therapies by 2020. Pharmacogenetics: A dream that will come trueThe integration of pharmacogenetics to pain therapy in an effort to improve pain management by individualization of therapy might sound overly optimistic today. Yet with continuous improvements in genomic technology and single nucleotide polymorphism (SNP) screening and identification, it is not unexpected that screening for specific SNPs before deciding the treatment plan for pain would become as routine as measuring platelets count before prescribing heparin is routine nowadays. We have shown that variations in the gene expression of COX-2 as well as the analgesic efficacy of the non-steroidal antiinflammatory drug ibuprofen and the selective COX-2 inhibitor rofecoxib are functionally associated with a SNP in PTGS2 [3]. Others have shown variability in morphine pain relief associated with genetic polymorphism [4,5]. Further, polymorphisms affecting drugmetabolizing enzymes and drug transporters that impact the pharmacokinetics of some drugs

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N‐Methyl‐D‐aspartate Antagonists and Neuropathic Pain: The Search for Relief.

Abstract: ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.

Cited by 24 publications

References 1 publication

Targeting the NMDA Receptor Subunit NR2B for the Treatment of Neuropathic Pain

Targeting the NMDA Receptor Subunit NR2B for the Treatment of Neuropathic Pain

Colorimetric chiral fluorescent sensors for Eu³⁺ and sequential enantioselective sensing of malate anion

2020 foresight: Envisioning therapeutic innovations for pain

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N‐Methyl‐D‐aspartate Antagonists and Neuropathic Pain: The Search for Relief.

Abstract: ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.

Cited by 24 publications

References 1 publication

Targeting the NMDA Receptor Subunit NR2B for the Treatment of Neuropathic Pain

Targeting the NMDA Receptor Subunit NR2B for the Treatment of Neuropathic Pain

Colorimetric chiral fluorescent sensors for Eu3+ and sequential enantioselective sensing of malate anion

2020 foresight: Envisioning therapeutic innovations for pain

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Product

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Colorimetric chiral fluorescent sensors for Eu³⁺ and sequential enantioselective sensing of malate anion