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GAL-021研究进展

发布日期：2017-10-30   浏览次数：0
核心提示：a href=https://www.medchemexpress.com/GAL-021.htmlGAL-021/a产品描述：GAL-021 a new intravenous bBKCa-channel/b blocker.i
<a href="https://www.medchemexpress.com/GAL-021.html">GAL-021</a>产品描述：GAL-021 a new intravenous <b>BKCa-channel</b> blocker.

<i><b>In Vitro:</b></i> GAL-021 is being developed as a novel breathing control modulator to preserve respiratory drive and protect patients from respiratory impairment due to opioids and other modalities. Using inside-out patches in GH3 cells, GAL-021 exerts concentration-dependent inhibition of single-channel KCa1.1 activity. When evaluated against 12 different cardiac ion channels, inhibition is 35% or less at 30 μM. No significant kinase inhibition is observed at 10 μM. At 30 μM in the radioligand binding assays, interactions (defined as >50% radioligand displacement) are detected at adenosine A1 (65% I), A2A (79% I, IC<sub>50</sub> approximately 5μM), and A3 (93% I; IC<sub>50</sub> approximately 1 μM) receptors, at 5-HT2B receptors (60% I; IC<sub>50</sub> approximately 30 μM)<sup>[1]</sup>.



<i><b>In Vivo:</b></i> Intravenously administered GAL-021 attenuates opiate-induced respiratory depression in rats and nonhuman prima<br><br>
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