Structure, function, and pharmacology of glutamate receptor ion channels

KB Hansen, LP Wollmuth, D Bowie, H Furukawa… - Pharmacological …, 2021 - ASPET
Many physiologic effects of l-glutamate, the major excitatory neurotransmitter in the
mammalian central nervous system, are mediated via signaling by ionotropic glutamate …

Novel rapid-acting glutamatergic modulators: targeting the synaptic plasticity in depression

YT Wang, XL Wang, ST Feng, NH Chen… - Pharmacological …, 2021 - Elsevier
Major depressive disorder (MDD) is severely prevalent, and conventional monoaminergic
antidepressants gradually exhibit low therapeutic efficiency, especially for patients with …

Investigational drugs in recent clinical trials for treatment-resistant depression

RP Garay, CA Zarate Jr, T Charpeaud… - Expert review of …, 2017 - Taylor & Francis
Introduction: The authors describe the medications for treatment-resistant depression (TRD)
in phase II/III of clinical development in the EU and USA and provide an opinion on how …

Ketamine in the past, present, and future: mechanisms, metabolites, and toxicity

ES Schwenk, B Pradhan, R Nalamasu, L Stolle… - Current pain and …, 2021 - Springer
Abstract Purpose of Review While ketamine's analgesia has mostly been attributed to
antagonism of N-methyl-d-aspartate receptors, evidence suggests multiple other pathways …

Beyond ketamine: new approaches to the development of safer antidepressants

S Chaki - Current neuropharmacology, 2017 - ingentaconnect.com
Background: Ketamine has been reported to exert rapid and sustained antidepressant
effects in patients with depression, including patients with treatment-resistant depression …

Structure–Affinity Relationships of 2,3,4,5-Tetrahydro-1H-3-benzazepine and 6,7,8,9-Tetrahydro-5H-benzo[7]annulen-7-amine Analogues and the Discovery of a Radiofluorinated 2,3,4,5-Tetrahydro …

H Ahmed, A Haider, J Varisco… - Journal of medicinal …, 2019 - ACS Publications
Aspiring to develop a positron emission tomography (PET) imaging agent for the GluN2B
subunits of the N-methyl-d-aspartate receptor (NMDAR), a key therapeutic target for drug …

Preclinical evaluation of benzazepine-based PET radioligands (R)-and (S)-11C-Me-NB1 reveals distinct enantiomeric binding patterns and a tightrope walk between …

A Haider, AM Herde, SD Krämer, J Varisco… - Journal of Nuclear …, 2019 - Soc Nuclear Med
The study aims to investigate the performance characteristics of the enantiomers of 11C-Me-
NB1, a recently reported PET imaging probe that targets the GluN2B subunit of N-methyl-d …

Rislenemdaz treatment in the lateral habenula improves despair-like behavior in mice

T Lei, D Dong, M Song, Y Sun, X Liu… - …, 2020 - nature.com
The specific GluN2B antagonist rislenemdaz (Ris; aka MK-0657 and CERC-301) is in phase
II clinical trial as an antidepressive drug, but the working mechanism for its antidepressant …

Enhanced attention and impulsive action following NMDA receptor GluN2B-selective antagonist pretreatment

GA Higgins, LB Silenieks, C MacMillan, J Sevo… - Behavioural brain …, 2016 - Elsevier
Abstract NMDA GluN2B (NR2B) subtype selective antagonists are currently in clinical
development for a variety of indications, including major depression. We previously reported …

Beyond serotonin: newer antidepressants in the future

G Rakesh, CU Pae, PS Masand - Expert Review of …, 2017 - Taylor & Francis
Introduction: There are numerous antidepressants for the treatment of major depressive
disorder (MDD) on the market. However, inadequate treatment response, therapeutic lag …