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Silodosin研究進(jìn)展

發(fā)布日期：2017-10-27   瀏覽次數(shù)：0
核心提示：a href=https://www.medchemexpress.com/Silodosin.htmlSilodosin/a產(chǎn)品描述：Silodosin (Rapaflo; KMD-3213) is an 1-adrenocep
<a href="https://www.medchemexpress.com/Silodosin.html">Silodosin</a>產(chǎn)品描述：Silodosin (Rapaflo; KMD-3213) is an α1-adrenoceptor antagonist with high uroselectivity; In treatment of dysuria.

IC50 Value:

Target: Adrenergic Receptor

in vitro: Silodosin potently inhibited 2-[2-(4-hydroxy-3-[125I]iodophenyl)ethylaminomethyl]-alpha-tetralone binding to the cloned human alpha 1a-AR, with a Ki value of 0.036 nM, but had 583- and 56-fold lower potency at the alpha 1b- and alpha 1d-ARs, respectively. Silodosin inhibited norepinephrine-induced increases in intracellular Ca2+ concentrations in alpha 1a-AR-expressing Chinese hamster ovary cells with an IC50 of 0.32 nM but had a much weaker inhibitory effect on the alpha 1b- and alpha 1d-ARs.

in vivo: Using pharmacologically well characterized native rat tissues [submaxillary gland (alpha 1A-AR-expressing tissue), liver (alpha 1B-AR-expressing tissue), and heart (mixed alpha 1A- and alpha 1B-AR-expressing tissue)], binding studies showed that inhibition curves for Silodosin in submaxillary gland and liver best fit a on<br><br>
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已為全球多個(gè)知名企業(yè)、院校構(gòu)建各種定制型化合物庫(kù)。</span><br><br>產(chǎn)品鏈接：<a href="http://www.medchemexpress.cn/silodosin.html">www.medchemexpress.cn/silodosin.html</a><br><br></span><img style="width: 600.0px;height: 310.0px;"

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