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

Autor: 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

Publikováno v: Kickinger, S, Lie, M E K, Suemasa, A, Al-Khawaja, A, Fujiwara, K, Watanabe, M, Wilhelmsen, K S, Falk-Petersen, C B, Frølund, B, Shuto, S, Ecker, G F & Wellendorph, P 2021, ' Molecular Determinants and Pharmacological Analysis for a Class of Competitive Non-transported Bicyclic Inhibitors of the Betaine/GABA Transporter BGT1 ', Frontiers in Chemistry, vol. 9, 736457 . https://doi.org/10.3389/fchem.2021.736457

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 pharmacolog

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Structure-Activity Studies of 3,9-Diazaspiro[5.5]undecane-Based γ-Aminobutyric Acid Type A Receptor Antagonists with Immunomodulatory Effect.

Autor: Bavo, Francesco, de-Jong, Heleen, Petersen, Jonas, Falk-Petersen, Christina Birkedahl, Löffler, Rebekka, Sparrow, Emma, Rostrup, Frederik, Eliasen, Jannik Nicklas, Wilhelmsen, Kristine S., Barslund, Kasper, Bundgaard, Christoffer, Nielsen, Birgitte, Kristiansen, Uffe, Wellendorph, Petrine, Bogdanov, Yury, Frølund, Bente

Publikováno v: Journal of Medicinal Chemistry; 12/23/2021, Vol. 64 Issue 24, p17795-17812, 18p