On March 14, 2019, Krall, Jacob; Bavo, Francesco; Falk-Petersen, Christina B.; Jensen, Claus H.; Nielsen, Julie O.; Tian, Yongsong; Anglani, Valeria; Kongstad, Kenneth T.; Piilgaard, Louise; Nielsen, Birgitte; Gloriam, David E.; Kehler, Jan; Jensen, Anders A.; Harpsoee, Kasper; Wellendorph, Petrine; Froelund, Bente published an article.Name: tert-Butyl trichloroacetimidate The title of the article was Discovery of 2-(Imidazo[1,2-b]pyridazin-2-yl)acetic acid as a new class of ligands selective for the γ-hydroxybutyric acid (GHB) high-affinity binding sites. And the article contained the following:
Gabazine, a γ-aminobutyric acid type A (GABAA) receptor antagonist, has previously been reported to inhibit the binding of [3H]NCS-382, a representative ligand of the high-affinity binding site for the neuroactive substance γ-hydroxybutyric acid (GHB). We herein report a study on the structural determinants of gabazine for binding to (i) the orthosteric binding site of the GABAA receptor and (ii) the high-affinity GHB binding site. Expanding the structural diversity of available ligands for the high-affinity GHB binding sites, this study identified 2-(imidazo[1,2-b]pyridazin-2-yl)acetic acid as a novel ligand-scaffold leading to analogs with relatively high affinity (Ki 0.19-2.19 μM) and >50 times selectivity for the [3H]NCS-382 over [3H]muscimol binding sites. These results highlight that gabazine interacts with the high-affinity GHB and orthosteric GABAA receptor binding sites differently and that distinct analogs can be generated to select between them. To facilitate further in vivo studies, a promising prodrug candidate for brain delivery was identified. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Name: tert-Butyl trichloroacetimidate
The Article related to gabazine gamma hydroxybutyric acid high affinity binding site gabaa, Pharmacology: Structure-Activity and other aspects.Name: tert-Butyl trichloroacetimidate
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