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DREADD agonist 21

发布日期：2017-10-26   浏览次数：0
核心提示：a href=https://www.medchemexpress.com/DREADD-agonist-21.htmlDREADD agonist 21/a产品描述：DREADD agonist 21 is a potent h
<a href="https://www.medchemexpress.com/DREADD-agonist-21.html">DREADD agonist 21</a>产品描述：DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptors (<b>hM3Dq</b>) agonist(<b>EC<sub>50</sub></b>=1.7 nM).

IC50 & Target: EC50: 1.7 nM (hM3Dq)<sup>[1]</sup><br/>Ki: 6 nM (H1 histamine receptor), 66 nM (5HT2A serotonin receptor 5HT2A), 170 nM (5HT2C serotonin receptor), 280 nM (α1A adrenergic receptor)<sup>[1]</sup>

<i><b>In Vitro:</b></i> DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist (EC<sub>50</sub>=1.7 nM) and does not activate human M3 receptor (hM3). In addition to being inactive at hM3, DREADD agonist 21, a potent full agonist of hM3Dq (EC<sub>50</sub>=1.7 nM), is only 3.5-fold selective for hM3Dq over H1, 40-fold selective over 5HT2A, 100-fold selective over 5HT2C, and 165-fold selective over α1A. DREADD agonist 21 shows high binding affinities to 5HT2A and 5HT2C serotonin receptor, α1A adrenergic receptor, and H1 histamine receptor with K<sub>i</sub> values of 66, 170, 280, and 6 nM, respectively<sup>[1]</sup><br><br>
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