Bioavailability Studies and in vitro Profiling of the Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitor UCPH-102

Autor: Anette L. Eriksen, Stinne W. Hansen, Josep A. Ruiz, Christoffer Bundgaard, Jesper F. Bastlund, Isabell Haym, Bjarke Abrahamsen, Anders A. Jensen, Lennart Bunch, Mikko Gynther, Tri H. V. Huynh, Mette N. Erichsen, Walden E. Bjørn-Yoshimoto, Martin Holst Friborg Pedersen

Publikováno v: ChemMedChem. 11:403-419

Although the selective excitatory amino acid transporter subtype 1 (EAAT1) inhibitor UCPH-101 has become a standard pharmacological tool compound for in vitro and ex vivo studies in the EAAT research field, its inability to penetrate the blood-brain

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6d0f875dae7a0b00cd26818da7ddad1a
https://doi.org/10.1002/cmdc.201500527

Design, synthesis and pharmacological characterization of coumarin-based fluorescent analogs of excitatory amino acid transporter subtype 1 selective inhibitors, UCPH-101 and UCPH-102

Autor: Bjarke Abrahamsen, Karsten K. Madsen, Anders A. Jensen, Alba Gonzalez-Franquesa, Lennart Bunch, Tri H. V. Huynh

Publikováno v: Bioorganic & Medicinal Chemistry. 20:6831-6839

The excitatory amino acid transporters (EAATs) play a pivotal role in regulating the synaptic concentration of glutamate in the mammalian central nervous system. To date, five different subtypes have been identified, named EAAT15 in humans (and GLAST

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1f5365985b373f427c4a0565fbb2b101
https://doi.org/10.1016/j.bmc.2012.09.049

Structure–Activity Relationship Study of Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitor 2-Amino-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile (UCPH-101) and Absolute Configurational Assignment Using Infrared and Vibrational Circular Dichroism Spectroscopy in Combination with ab Initio Hartree–Fock Calculations

Autor: Anders A. Jensen, Henrik Bohr, Irene Shim, Birgitte Nielsen, Lennart Bunch, Bjarke Abrahamsen, Tri H. V. Huynh

Publikováno v: Huynh, T H V, Shim, I, Bohr, H, Abrahamsen, B, Nielsen, B, Jensen, A A & Bunch, L 2012, ' Structure–Activity Relationship Study of Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitor 2-Amino-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile (UCPH-101) and Absolute Configurational Assignment Using Infrared and Vibrational Circular Dichroism Spectroscopy in Combination with ab Initio Hartree–Fock Calculations ', Journal of Medicinal Chemistry, vol. 55, no. 11, pp. 5403-5412 . https://doi.org/10.1021/jm300345z

The excitatory amino acid transporters (EAATs) play essential roles in regulating the synaptic concentration of the neurotransmitter glutamate in the mammalian central nervous system. To date, five subtypes have been identified, named EAAT1–5 in hu

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::064e44b0e5843f324e9ce3a4348043f9
https://doi.org/10.1021/jm300345z

A Versatile Approach to β-Amyloid Fibril-Binding Compounds Exploiting the Shirakawa/Hayashi Protocol for trans-Alkene Synthesis

Autor: Anders T. Lindhardt, Tri H. V. Huynh, Niels Chr. Nielsen, Daniel E. Otzen, Troels Skrydstrup, Katrine Mikkelsen, Mette Louise H. Mantel

Publikováno v: Organic Letters. 11:999-1002

Application of the Sonogashira coupling reaction followed by a trans-selective alkyne reduction proved highly adaptable for the efficient synthesis of a class of beta-amyloid fibril binding compounds possessing a styrylbenzene motif such as FSB, an F

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3575d7b2ec3c22f710ed45ac7ac7f541
https://doi.org/10.1021/ol8029593

Profiling substrate specificity of two series of phenethylamine analogs at monoamine oxidase A and B

Autor: Egon Heuson, Morten Storgaard, Lennart Bunch, Tri H. V. Huynh, Thierry Gefflaut, Franck Charmantray

Publikováno v: Organic and Biomolecular Chemistry
Organic and Biomolecular Chemistry, Royal Society of Chemistry, 2014, 12, pp.8689-8695. ⟨10.1039/C4OB01377H⟩
Organic & Biomolecular Chemistry
Organic & Biomolecular Chemistry, Royal Society of Chemistry, 2014, 12, pp.8689-8695. ⟨10.1039/C4OB01377H⟩

International audience; The membrane bound enzyme monoamine oxidase exist in two splice variants designated A and B (MAO-A and MAO-B) and are key players in the oxidative metabolism of monoamines in mammalians. Despite their importance and being a pr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1203e08f8b26dfe20b52325bf3f2281a
https://hal.archives-ouvertes.fr/hal-01099212