Cargando…

Molecular Determinants and Pharmacological Analysis for a Class of Competitive Non-transported Bicyclic Inhibitors of the Betaine/GABA Transporter BGT1

The betaine/GABA transporter 1 (BGT1) is a member of the GABA transporter (GAT) family with still elusive function, largely due to a lack of potent and selective tool compounds. Based on modeling, we here present the design, synthesis and pharmacological evaluation of five novel conformationally res...

Descripción completa

Detalles Bibliográficos
Autores principales:	Kickinger, Stefanie, Lie, Maria E. K., Suemasa, Akihiro, Al-Khawaja, Anas, Fujiwara, Koichi, Watanabe, Mizuki, Wilhelmsen, Kristine S., Falk-Petersen, Christina B., Frølund, Bente, Shuto, Satoshi, Ecker, Gerhard F., Wellendorph, Petrine
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	Frontiers Media S.A. 2021
Materias:	Chemistry
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8476755/ https://www.ncbi.nlm.nih.gov/pubmed/34595152 http://dx.doi.org/10.3389/fchem.2021.736457

Ejemplares similares

Exploring the molecular determinants for subtype-selectivity of 2-amino-1,4,5,6-tetrahydropyrimidine-5-carboxylic acid analogs as betaine/GABA transporter 1 (BGT1) substrate-inhibitors
por: Kickinger, Stefanie, et al.
Publicado: (2020)

Pharmacological Characterization of a Betaine/GABA Transporter 1 (BGT1) Inhibitor Displaying an Unusual Biphasic Inhibition Profile and Anti-seizure Effects
por: Lie, Maria E. K., et al.
Publicado: (2020)

Inhibitory Action of Antidepressants on Mouse Betaine/GABA Transporter (BGT1) Heterologously Expressed in Cell Cultures
por: Gerile,, et al.
Publicado: (2012)

The betaine/GABA transporter and betaine: roles in brain, kidney, and liver
por: Kempson, Stephen A., et al.
Publicado: (2014)

Discovery of a new class of orthosteric antagonists with nanomolar potency at extrasynaptic GABA(A) receptors
por: Falk-Petersen, Christina Birkedahl, et al.
Publicado: (2020)

Effects of betaine on lipopolysaccharide-induced memory impairment in mice and the involvement of GABA transporter 2
por: Miwa, Masaya, et al.
Publicado: (2011)

Pharmacological characterisation of murine α4β1δ GABA(A) receptors expressed in Xenopus oocytes
por: Villumsen, Inge S, et al.
Publicado: (2015)

The Binding of Alpinia galanga Oil and Its Nanoemulsion to Mammal GABA(A) Receptors Using Rat Cortical Membranes and an In Silico Modeling Platform
por: Khumpirapang, Nattakanwadee, et al.
Publicado: (2022)

The implementation results of safe bicycle transport in Taipei City
por: Yin-Huan, Wu, et al.
Publicado: (2019)

GABA and Glutamate Transporters in Brain
por: Zhou, Yun, et al.
Publicado: (2013)

Anion transport and GABA signaling
por: Hübner, Christian A., et al.
Publicado: (2013)

CaMKIIα as a Promising Drug Target for Ischemic Grey Matter
por: Griem-Krey, Nane, et al.
Publicado: (2022)

Visuospatial working memory abilities in children analyzed by the bricks game task (BGT)
por: D’Aurizio, G., et al.
Publicado: (2023)

Structure, function, and plasticity of GABA transporters
por: Scimemi, Annalisa
Publicado: (2014)

Reconstitution of GABA, Glycine and Glutamate Transporters
por: Danbolt, Niels Christian, et al.
Publicado: (2021)

The impact of transportation infrastructure on bicycling injuries and crashes: a review of the literature
por: Reynolds, Conor CO, et al.
Publicado: (2009)

A comparative review on the well-studied GAT1 and the understudied BGT-1 in the brain
por: Bhatt, Manan, et al.
Publicado: (2023)

Synthesis and Pharmacological Evaluation of [(11)C]4-Methoxy-N-[2-(thiophen-2-yl)imidazo[1,2-a]pyridin-3-yl]benzamide as a Brain Penetrant PET Ligand Selective for the δ-Subunit-Containing γ-Aminobutyric Acid Type A Receptors
por: L’Estrade, Elina T., et al.
Publicado: (2019)

GABA Metabolism and Transport: Effects on Synaptic Efficacy
por: Roth, Fabian C., et al.
Publicado: (2012)

Characteristic Expressions of GABA Receptors and GABA Producing/Transporting Molecules in Rat Kidney
por: Takano, Kozue, et al.
Publicado: (2014)

Bicycle ownership and utilization in Tamale Metropolis; influencing factors and impacts to sustainable transport
por: Timpabi, Akua Pokuaa, et al.
Publicado: (2021)

A functional role for both γ-aminobutyric acid (GABA) transporter-1 and GABA transporter-3 in the modulation of extracellular GABA and GABAergic tonic conductances in the rat hippocampus
por: Kersanté, Flavie, et al.
Publicado: (2013)

Cryo-EM structure of GABA transporter 1 reveals substrate recognition and transport mechanism
por: Nayak, Smruti Ranjan, et al.
Publicado: (2023)

Astrocytic GABA transporter activity modulates excitatory neurotransmission
por: Boddum, Kim, et al.
Publicado: (2016)

Bicycle Use for Transport in an Australian and a Belgian City: Associations with Built-Environment Attributes
por: Owen, Neville, et al.
Publicado: (2010)

Buses, Cars, Bicycles and Walkers: The Influence of the Type of Human Transport on the Flight Responses of Waterbirds
por: McLeod, Emily M., et al.
Publicado: (2013)

Perceived Social and Built Environment Correlates of Transportation and Recreation-Only Bicycling Among Adults
por: Porter, Anna K., et al.
Publicado: (2018)

Health economic assessment of a scenario to promote bicycling as active transport in Stockholm, Sweden
por: Kriit, Hedi Katre, et al.
Publicado: (2019)

Perception of the purchase budget (BGT) and purchase intention in smartphone selling industry: A cross-country analysis
por: N’da, Karamoko, et al.
Publicado: (2023)

Insights into binding events of GABA- and Tiagabine- analogues in the Gamma-Aminobutyric Acid Transporter 1 by means of Molecular Modelling
por: Zdrazil, Barbara, et al.
Publicado: (2012)

GABA transporter sustains IL-1β production in macrophages
por: Xia, Yaoyao, et al.
Publicado: (2021)

Synaptic GABA release prevents GABA transporter type-1 reversal during excessive network activity
por: Savtchenko, Leonid, et al.
Publicado: (2015)

Functional characterization of GABA(A) receptor-mediated modulation of cortical neuron network activity in microelectrode array recordings
por: Bader, Benjamin M., et al.
Publicado: (2017)

Feasibility of a blended group treatment (bGT) for major depression: uncontrolled interventional study in a university setting
por: Schuster, Raphael, et al.
Publicado: (2018)

Limitations of Current GABA Agonists in Neonatal Seizures: Toward GABA Modulation Via the Targeting of Neuronal Cl(−) Transport
por: Khanna, Arjun, et al.
Publicado: (2013)

Glutamate Uptake Triggers Transporter-Mediated GABA Release from Astrocytes
por: Héja, László, et al.
Publicado: (2009)

Inhibition of Activity of GABA Transporter GAT1 by δ-Opioid Receptor
por: Pu, Lu, et al.
Publicado: (2012)

Plasticity of GABA transporters: an unconventional route to shape inhibitory synaptic transmission
por: Scimemi, Annalisa
Publicado: (2014)

GABA Transporter-1 Deficiency Confers Schizophrenia-Like Behavioral Phenotypes
por: Yu, Zhe, et al.
Publicado: (2013)

Characterizing the transport and utilization of the neurotransmitter GABA in the bacterial pathogen Brucella abortus
por: Budnick, James A., et al.
Publicado: (2020)

Cannot write session to /tmp/vufind_sessions/sess_r2h6utkga2s4euofhimi1l4mo8