Cargando…

Strong Inhibitory Effect, Low Cytotoxicity and High Plasma Stability of Steroidal Inhibitors of N-Methyl-D-Aspartate Receptors With C-3 Amide Structural Motif

Herein, we report the synthesis, structure-activity relationship study, and biological evaluation of neurosteroid inhibitors of N-methyl-D-aspartate receptors (NMDARs) receptors that employ an amide structural motif, relative to pregnanolone glutamate (PAG) – a compound with neuroprotective properti...

Descripción completa

Detalles Bibliográficos
Autores principales:	Adla, Santosh Kumar, Slavikova, Barbora, Chodounska, Hana, Vyklicky, Vojtech, Ladislav, Marek, Hubalkova, Pavla, Krausova, Barbora, Smejkalova, Tereza, Nekardova, Michaela, Smidkova, Marketa, Monincova, Lenka, Soucek, Radko, Vyklicky, Ladislav, Kudova, Eva
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	Frontiers Media S.A. 2018
Materias:	Pharmacology
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6240685/ https://www.ncbi.nlm.nih.gov/pubmed/30483134 http://dx.doi.org/10.3389/fphar.2018.01299

Ejemplares similares

Pitfalls of NMDA Receptor Modulation by Neuroactive Steroids. The Effect of Positive and Negative Modulation of NMDA Receptors in an Animal Model of Schizophrenia
por: Holubova, Kristina, et al.
Publicado: (2021)

Surface Expression, Function, and Pharmacology of Disease-Associated Mutations in the Membrane Domain of the Human GluN2B Subunit
por: Vyklicky, Vojtech, et al.
Publicado: (2018)

Endogenous neurosteroids pregnanolone and pregnanolone sulfate potentiate presynaptic glutamate release through distinct mechanisms
por: Smejkalova, Tereza, et al.
Publicado: (2021)

Block of NMDA receptor channels by endogenous neurosteroids: implications for the agonist induced conformational states of the channel vestibule
por: Vyklicky, Vojtech, et al.
Publicado: (2015)

Cholesterol modulates presynaptic and postsynaptic properties of excitatory synaptic transmission
por: Korinek, Miloslav, et al.
Publicado: (2020)

The LILI Motif of M3-S2 Linkers Is a Component of the NMDA Receptor Channel Gate
por: Ladislav, Marek, et al.
Publicado: (2018)

Distinct regions within the GluN2C subunit regulate the surface delivery of NMDA receptors
por: Lichnerova, Katarina, et al.
Publicado: (2014)

PM335. Neuroactive steroid treatment in the model of focal cerebra ischemia in immature brain
por: Vales, K., et al.
Publicado: (2016)

NMDA Receptor Opening and Closing—Transitions of a Molecular Machine Revealed by Molecular Dynamics
por: Černý, Jiří, et al.
Publicado: (2019)

Neurogenesis as a Tool for Spinal Cord Injury
por: Havelikova, Katerina, et al.
Publicado: (2022)

Conformational rearrangement of the NMDA receptor amino-terminal domain during activation and allosteric modulation
por: Vyklicky, Vojtech, et al.
Publicado: (2021)

The Neuroactive Steroid Pregnanolone Glutamate: Anticonvulsant Effect, Metabolites and Its Effect on Neurosteroid Levels in Developing Rat Brains
por: Kudova, Eva, et al.
Publicado: (2021)

Evidence for the Association between the Intronic Haplotypes of Ionotropic Glutamate Receptors and First-Episode Schizophrenia
por: Hirschfeldova, Katerina, et al.
Publicado: (2021)

Catechins Variously Affect Activities of Conjugation Enzymes in Proliferating and Differentiated Caco-2 Cells
por: Lněničková, Kateřina, et al.
Publicado: (2016)

Effect of Standardized Cranberry Extract on the Activity and Expression of Selected Biotransformation Enzymes in Rat Liver and Intestine
por: Bártíková, Hana, et al.
Publicado: (2014)

High-entropy oxychloride increasing the stability of Li–sulfur batteries
por: Zukalová, Markéta, et al.
Publicado: (2023)

Tailor-Made Immunochromatographic Test for the Detection of Multiple 17α-Methylated Anabolics in Dietary Supplements
por: Holubová, Barbora, et al.
Publicado: (2021)

Exon First Nucleotide Mutations in Splicing: Evaluation of In Silico Prediction Tools
por: Grodecká, Lucie, et al.
Publicado: (2014)

Conformational pathway provides unique sensitivity to a synaptic mGluR
por: Habrian, Chris H., et al.
Publicado: (2019)

Interleukin 35 Synovial Fluid Levels Are Associated with Disease Activity of Rheumatoid Arthritis
por: Šenolt, Ladislav, et al.
Publicado: (2015)

In Vivo Bioavailability of Selenium in Selenium-Enriched Streptococcus thermophilus and Enterococcus faecium in CD IGS Rats
por: Krausova, Gabriela, et al.
Publicado: (2021)

Functional Properties of Dunaliella salina and Its Positive Effect on Probiotics
por: Hyrslova, Ivana, et al.
Publicado: (2022)

Prognostic Importance of Cell Cycle Regulators Cyclin D1 (CCND1) and Cyclin-Dependent Kinase Inhibitor 1B (CDKN1B/p27) in Sporadic Gastric Cancers
por: Minarikova, Petra, et al.
Publicado: (2016)

Camptothecin, triptolide, and apoptosis inducer kit have differential effects on mitochondria in colorectal carcinoma cells
por: Liskova, Veronika, et al.
Publicado: (2022)

Membrane Proteins and Proteomics of Cronobacter sakazakii Cells: Reliable Method for Identification and Subcellular Localization
por: Novotný, Jiří, et al.
Publicado: (2022)

Involvement of mTOR Pathways in Recovery from Spinal Cord Injury by Modulation of Autophagy and Immune Response
por: Vargova, Ingrid, et al.
Publicado: (2021)

Relational and interactional dynamic network data from Czech lower-secondary school students
por: Lintner, Tomáš, et al.
Publicado: (2023)

S100A4 is elevated in axial spondyloarthritis: a potential link to disease severity
por: Šumová, Barbora, et al.
Publicado: (2020)

Inhibition of Hsp90 Counteracts the Established Experimental Dermal Fibrosis Induced by Bleomycin
por: Štorkánová, Hana, et al.
Publicado: (2021)

Correction: Štorkánová et al. Inhibition of Hsp90 Counteracts the Established Experimental Dermal Fibrosis Induced by Bleomycin. Biomedicines 2021, 9, 650
por: Štorkánová, Hana, et al.
Publicado: (2023)

Modulatory effect of MG-132 proteasomal inhibition on boar sperm motility during in vitro capacitation
por: Hackerova, Lenka, et al.
Publicado: (2023)

Female Sexual Dysfunction and Pelvic Floor Muscle Function Associated with Systemic Sclerosis: A Cross-Sectional Study
por: Heřmánková, Barbora, et al.
Publicado: (2022)

Poly-N-Acetyllactosamine Neo-Glycoproteins as Nanomolar Ligands of Human Galectin-3: Binding Kinetics and Modeling
por: Bumba, Ladislav, et al.
Publicado: (2018)

Unmeasurable capillary C-reactive protein as one of the diagnostic clues of severe hematological pathologies in children in primary settings: Case series
por: Piteková, Barbora, et al.
Publicado: (2023)

Structural features in the glycine-binding sites of the GluN1 and GluN3A subunits regulate the surface delivery of NMDA receptors
por: Skrenkova, Kristyna, et al.
Publicado: (2019)

Autosomal recessive limb-girdle muscular dystrophies in the Czech Republic
por: Stehlíková, Kristýna, et al.
Publicado: (2014)

Neurosteroids: Structure-Uptake Relationships and Computational Modeling of Organic Anion Transporting Polypeptides (OATP)1A2
por: Adla, Santosh Kumar, et al.
Publicado: (2021)

Phenotypic Heterogeneity of Triple-Negative Breast Cancer Mediated by Epithelial–Mesenchymal Plasticity
por: Kvokačková, Barbora, et al.
Publicado: (2021)

In Vitro Selective Antibacterial and Antiproliferative Effects of Ethanolic Extracts from Cambodian and Philippine Plants Used in Folk Medicine for Diarrhea Treatment
por: Kudera, Tomas, et al.
Publicado: (2021)

Effect of an 8-Week Tailored Physiotherapy Program on Sexual Health in Women with Scleroderma and Myositis: A Controlled Pilot Study
por: Heřmánková, Barbora, et al.
Publicado: (2023)

Cannot write session to /tmp/vufind_sessions/sess_fb96nlbq15e728mfdmq2ug3d6h