Abstract:
INTRODUCTION:The N-methyl-d-aspartate receptor-ionophore complex plays a key role in learning and memory and has efficacy in animals and humans with affective disorders. GLYX-13 is an N-methyl-d-aspartate receptor (NMDAR) glycine-site functional partial agonist and cognitive enhancer that also shows rapid antidepressant activity without psychotomimetic side effects. AREAS COVERED:The authors review the mechanism of action of GLYX-13 that was investigated in preclinical studies and evaluated in clinical studies. Specifically, the authors review its pharmacology, pharmacokinetics, and drug safety that were demonstrated in clinical studies. EXPERT OPINION:NMDAR full antagonists can produce rapid antidepressant effects in treatment-resistant subjects; however, they are often accompanied by psychotomimetic effects that make chronic use outside of a clinical trial inpatient setting problematic. GLYX-13 appears to exert its antidepressant effects in the frontal cortex via NMDAR-triggered synaptic plasticity. Understanding the mechanistic underpinning of GLYX-13's antidepressant action should provide both novel insights into the role of the glutamatergic system in depression and identify new targets for therapeutic development.
journal_name
Expert Opin Investig Drugsjournal_title
Expert opinion on investigational drugsauthors
Moskal JR,Burch R,Burgdorf JS,Kroes RA,Stanton PK,Disterhoft JF,Leander JDdoi
10.1517/13543784.2014.852536subject
Has Abstractpub_date
2014-02-01 00:00:00pages
243-54issue
2eissn
1354-3784issn
1744-7658journal_volume
23pub_type
杂志文章,评审abstract:INTRODUCTION:Current treatment for polycythemia vera (PV) is limited and primarily targets thrombosis risk. Agents targeting distinct mechanisms of action within myeloproliferation are undergoing clinical evaluation to optimize efficacy, improve tolerance and augment long term disease complications. AREA COVERED:This ...
journal_title:Expert opinion on investigational drugs
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abstract:INTRODUCTION:Relapsed/refractory multiple myeloma (rrMM) remains a difficult condition to treat despite the availability of new drugs. This review aims to provide evidence to guide physicians in the choice of salvage therapy in certain subgroups of patients. AREAS COVERED:The review attempts to present evidence-based ...
journal_title:Expert opinion on investigational drugs
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doi:10.1517/13543784.2011.575060
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abstract:BACKGROUND:In the past years the bone seeking radiopharmaceutical samarium lexidronam ((153)Sm-EDTMP) has been increasingly used alone or in conjunction with chemotherapy and/or bisphosphonates for the treatment of painful bone metastasis. OBJECTIVE:Its use has been explored in different solid tumours. In this report ...
journal_title:Expert opinion on investigational drugs
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doi:10.1517/13543784.17.9.1379
更新日期:2008-09-01 00:00:00
abstract::ATP-gated P2X7 receptors (P2X7) make a unique family of extracellular ATP-activated plasma membrane ion channels expressed in haematopoietic and epithelial cells. They have been extensively studied in immune cells where their activation leads to the rapid release of pro-inflammatory cytokines and the initiation of the...
journal_title:Expert opinion on investigational drugs
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abstract:BACKGROUND:Armodafinil is a wake-promoting agent developed by Cephalon that was approved in mid-2007 for the treatment of excessive sleepiness associated with narcolepsy, obstructive sleep apnea and shift work disorder. It is the R-enantiomer of the compound modafinil. Like modafinil, the mechanism of action for armoda...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.17.4.565
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abstract::Increasing evidence suggests an important role for autocrine/paracrine prolactin in breast and prostate cancers and other disease states. Prolactin production in these extrapituitary sites is not governed by dopamine agonists, a finding that has spurred the production of prolactin receptor antagonists. This review foc...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
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journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
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journal_title:Expert opinion on investigational drugs
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journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.2014.934806
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abstract::'Male factor' problems contribute to subfertility in a significant proportion of couples. In some instances, defective sperm production has qualitative and/or quantitative effects on the semen profile; in others, no obvious defects can be detected, yet spermatozoa are non-fertilising. Recent studies have revealed that...
journal_title:Expert opinion on investigational drugs
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abstract::Presentations at the William Harvey Research Conference on PDE Inhibitors described the molecular biology, biochemical regulation. pharmacology, and therapeutic utility of inhibitors of cyclic nucleotide phosphodiesterases (PDEs). Most of the talks focused on PDE4 and PDE5. two members of the 11-member PDE family that...
journal_title:Expert opinion on investigational drugs
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journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
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更新日期:2000-09-01 00:00:00
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journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1517/13543784.6.8.1019
更新日期:1997-08-01 00:00:00
abstract:INTRODUCTION:Lupus nephritis (LN) is a significant contributor to morbidity and mortality in systemic lupus erythematosus (SLE). Current therapies for LN are limited by significant toxicities and high rates of relapse. A clear and present need exists for the development of effective, targeted and well-tolerated treatme...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
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journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
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更新日期:2015-01-01 00:00:00
abstract::Innate immune mechanisms respond rapidly to bacterial infection. A key cellular component of the innate immune response is the neutrophil, whose cytoplasmic granules contain a variety of antimicrobial proteins and peptides. Among these is the bactericidal/permeability-increasing protein (BPI), a cationic 55 kDa protei...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
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更新日期:2002-02-01 00:00:00
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journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1080/13543784.2020.1793955
更新日期:2020-09-01 00:00:00
abstract::Telomerase is a holoenzyme responsible for the maintenance of telomeres, the protein-nucleic acid complexes at the ends of eukaryotic chromosomes that serve to maintain chromosomal stability and integrity. Telomerase activity is essential for the sustained proliferation of most immortal cells, including cancer cells. ...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
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abstract:INTRODUCTION:Minimal change disease (MCD) and Focal and segmental glomerulosclerosis (FSGS) are two of the major causes of nephrotic syndrome (NS) in children and adults. According to KDIGO (Kidney Disease: Improving Global Outcomes) guidelines, the treatment of adult primary MCD and FSGS should be based on immunosuppr...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
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journal_title:Expert opinion on investigational drugs
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journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.2011.630660
更新日期:2011-12-01 00:00:00
abstract::PTI-821 is a long-acting formulation of oxycodone that is intended to deter abuse through its gel-cap technology. Produced by Pain Therapeutics in alliance with King Pharmaceuticals, PTI-821 is designed to provide strong pain relief with the intent of offering greater safety than is presently available from convention...
journal_title:Expert opinion on investigational drugs
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pub_type: 杂志文章,评审
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更新日期:2000-05-01 00:00:00
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journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
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更新日期:2007-01-01 00:00:00
abstract:IMPORTANCE OF THE FIELD:Contrasting with the broad activation of the PI3K/AKT/mammalian target of rapamycin (mTOR) survival pathway in most cancer, activity of rapalogues appears to be restricted to a few tumor types. AREAS COVERED IN THIS REVIEW:The analysis of molecular activity of the PI3K/AKT/mTOR pathway and resi...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.2010.499121
更新日期:2010-08-01 00:00:00
abstract:IMPORTANCE OF THE FIELD:Hepatitis C virus (HCV) is the main agent of chronic hepatitis, liver cirrhosis and hepatocellular carcinoma in the western world. It affects more than 170 million people worldwide. HCV treatment, based on the combination of Peg-interferon and ribavirin, is effective in about 50% of treated pati...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
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abstract:INTRODUCTION:In the last decade, concerns have been raised around the use of erythropoiesis-stimulating agents (ESAs) and intravenous iron in chronic kidney disease (CKD) patients, especially when given at high doses. Moreover, treatment with ESA is expensive. AREAS COVERED:We searched PubMed for original articles, re...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
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abstract::In most countries the last two decades have seen a very substantial rise in the prevalence of heart failure, and in a majority of patients hypertension is both an antecedent condition and a contributing cause. Heart failure is also a major cause of hospital admissions; its amelioration and, as far as possible, prevent...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
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更新日期:2003-12-01 00:00:00
abstract::Standard drug therapy of adult polymyositis, dermatomyositis and inclusion body myositis includes high-dose corticosteroids and cytotoxic drugs (methotrexate, azathioprine (AZA) and cyclophosphamide). Recent data are in favour of the early introduction of a cytotoxic or immunomodulating drug in addition to corticoster...
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abstract::Risperidone (Risperdal) is a benzisoxazole derivative with a high affinity for serotonin 5-HT2 and dopamine D2 receptors, and some affinity for alpha- adrenergic, histamine H1 and dopamine D1 receptors. It has no anticholinergic effects. Early studies demonstrated risperidone to be an effective medication for psychoti...
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