In 2010,Gao, Zhaobing; Zhang, Tangzhi; Wu, Meng; Xiong, Qiaojie; Sun, Haiyan; Zhang, Yinan; Zu, Liansuo; Wang, Wei; Li, Min published 《Isoform-specific Prolongation of Kv7 (KCNQ) Potassium Channel Opening Mediated by New Molecular Determinants for Drug-Channel Interactions》.Journal of Biological Chemistry published the findings.Product Details of 13534-97-9 The information in the text is summarized as follows:
Kv7 channels, especially Kv7.2 (KCNQ2) and Kv7.3 (KCNQ3), are key determinants for membrane excitability in the brain. Some chem. modulators of KCNQ channels are in development for use as anti-epileptic drugs, such as retigabine (D-23129, N-(2-amino-4-(4-fluorobenzylamino)-phenyl)), which was recently approved for clin. use. In addition, several other compounds were also reported to potentiate activity of the Kv7 channels. It is therefore of interest to investigate compound-channel interactions, so that more insights may be gained to aid future development of therapeutics. We have conducted a screen of 20,000 compounds for KCNQ2 potentiators using rubidium flux combined with at. absorption spectrometry. Here, we report the characterization of a series of new structures that display isoform specificity and induce a marked reduction of deactivation distinct from that of retigabine. Furthermore, KCNQ2(W236L), a previously reported mutation that abolishes sensitivity to retigabine, remains fully sensitive to these compounds This result, together with mutagenesis and other studies, suggests that the reported compounds confer a unique mode of action and involve new mol. determinants on the channel protein, consistent with the idea of recognizing a new site on channel protein. The results came from multiple reactions, including the reaction of 6-Bromopyridin-3-amine(cas: 13534-97-9Product Details of 13534-97-9)
6-Bromopyridin-3-amine(cas: 13534-97-9) belongs to anime. Reduction of nitro compounds, RNO2, by hydrogen or other reducing agents produces primary amines cleanly (i.e., without a mixture of products), but the method is mostly used for aromatic amines because of the limited availability of aliphatic nitro compounds. Reduction of nitriles and oximes (R2C=NOH) also yields primary amines.Product Details of 13534-97-9