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  4. L-654284

L-654284是一种α2-肾上腺素受体拮抗剂，具有明显的选择性。L-654284在体外与3H-clonidine和3H-rauwolscine的结合竞争，并分别显示出Ki值为0.8 nM和1.1 nM。L-654284能够阻断克隆尼定在大鼠孤立输精管中的前突效应，pA2值为9.1。L-654284在α2与α1肾上腺素受体选择性方面表现显著，在抑制3H-prazosin结合方面表现出Ki为110 nM。L-654284在体内能够显著增加大鼠脑皮层去甲肾上腺素周转率，显示中枢神经系统中α2-肾上腺素受体的阻断活性。

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L-654284 Chemical Structure

L-654284 Chemical Structure

CAS No. : 98719-20-1

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L-654284 相关抗体

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生物活性

L-654284 is an α2-adrenergic receptor antagonist with significant selectivity. L-654284 competes with the binding of 3H-clonidine and 3H-rauwolscine in vitro and shows Ki values of 0.8 nM and 1.1 nM, respectively. L-654284 can block the protrusion effect of clonidine in isolated vas deferens in rats, with a pA2 value of 9.1. L-654284 exhibits remarkable selectivity for α2 and α1 adrenergic receptors, and exhibits a Ki of 110 nM in inhibiting 3H-prazosin binding. L-654284 can significantly increase the turnover rate of norepinephrine in rat cerebral cortex in vivo, showing α2-adrenergic receptor blocking activity in the central nervous system[1].

分子量

364.46

Formula

C18H24N2O4S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

L-654284 相关分类

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Keywords:

L-65428498719-20-1L654284L 654284OthersInhibitorinhibitorinhibit

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产品名称：
L-654284
目录号：
HY-136693
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