3999-29-9Relevant articles and documents
Structural Determinants for the Mode of Action of Imidazopyridine DS2 at δ-Containing γ-Aminobutyric Acid Type A Receptors
Rostrup, Frederik,Falk-Petersen, Christina B.,Harpsoe, Kasper,Buchleithner, Stine,Conforti, Irene,Jung, Sascha,Gloriam, David E.,Schirmeister, Tanja,Wellendorph, Petrine,Frolund, Bente
, p. 4730 - 4743 (2021/05/06)
Despite the therapeutic relevance of δ-containing γ-aminobutyric acid type A receptors (GABAARs) and the need for δ-selective compounds, the structural determinants for the mode and molecular site of action of δ-selective positive allosteric modulator imi
Structure-Function Evaluation of Imidazopyridine Derivatives Selective for δ-Subunit-Containing γ-Aminobutyric Acid Type A (GABAA) Receptors
Yakoub, Kirsten,Jung, Sascha,Sattler, Christian,Damerow, Helen,Weber, Judith,Kretzschmann, Annika,Cankaya, Aylin S.,Piel, Markus,R?sch, Frank,Haugaard, Anne S.,Fr?lund, Bente,Schirmeister, Tanja,Lüddens, Hartmut
, p. 1951 - 1968 (2018/03/21)
δ-Selective compounds 1 and 2 (DS1, compound 22; DS2, compound 16) were introduced as functionally selective modulators of δ-containing GABA type A receptors (GABAAR). In our hands, [3H]EBOB-binding experiments with recombinant GABAAR and compound 22 showed no proof of δ-selectivity, although there was a minimally higher preference for the α4β3δ and α6β2/3δ receptors with respect to potency. In order to delineate the structural determinants of δ preferences, we synthesized 25 derivatives of DS1 and DS2, and investigated their structure-activity relationships (SAR). Four of our derivatives showed selectivity for α6β3δ receptors (29, 38, 39, and 41). For all of them, the major factors that distinguished them from compound 22 were variations at the para-positions of their benzamide groups. However, two compounds (29 and 39), when tested in the presence of GABA, revealed effects at several additional GABAAR. The newly synthesized compounds will still serve as useful tools to investigate α6β3δ receptors.
HETERO-CYCLIC COMPOUND AND ORGANIC LIGHT EMITTING DEVICE USING THE SAME
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Paragraph 0140; 0141; 0150; 0151, (2016/10/08)
The present specification relates to a novel heterocyclic compound and an organic light-emitting device using the same. According to one embodiment of the present specification, provided is a compound in chemical formula 1. The compound of the present specification can be used as an organic matter layer material of an organic light-emitting device.COPYRIGHT KIPO 2016