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PZM21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/PZM21.htmlPZM21/a产品描述：PZM21 is a potent and selective b opioid receptor/b ago
<a href="https://www.medchemexpress.com/PZM21.html">PZM21</a>产品描述：PZM21 is a potent and selective <b>μ opioid receptor</b> agonist with an <b>EC<sub>50</sub></b> of 1.8 nM.

IC50 & Target: EC50: 1.8 nM (μ opioid receptor)<sup>[1]</sup>

<i><b>In Vitro:</b></i> PZM21 has no detectable κOR or nociceptin receptor agonist activity-it is actually an 18 nM κOR antagonist-while it is a 500-fold weaker δOR agonist, making it a selective μOR agonist.  At hERG, PZM21 has an IC<sub>50</sub> of between 2 and 4 μM, 500- to 1,000-fold weaker than its potency as a μOR agonist. Signalling by PZM21 and other μOR agonists appears to be mediated primarily by the heterotrimeric G protein Gi/o, as its effect on cAMP levels is eliminated by pertussis toxin and no activity is observed in a calcium release assay <sup>[1]</sup>.

<i><b>In Vivo:</b></i> PZM21 is a potent Gi activator with exceptional selectivity for μOR and minimal β-arrestin-2 recruitment. Unlike morphine, PZM21 is more efficacious for the affective component of analgesia versus the reflexive component and <br><br>
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