LUF6096 是一种有效的腺苷 A3 受体 (adenosine A3 receptor) 变构增强剂。LUF6096 对任何腺苷受体显示出低正构亲和力。LUF6096 在心肌缺血/再灌注损伤中显示出保护作用。
LUF6096, a potent allosteric enhancer of the adenosine A3 receptor, is able to allosterically enhance agonist binding. LUF6096 shows low orthosteric affinity for any of the adenosine receptors. LUF6096 shows protective effects in myocardial ischemia/reperfusion injury[1][2].
LUF6096 (10 μM; 30-120 min) decreases the dissociation rate of 125I-AB-MECA from the A3 receptor by 2.5 times in CHO cell membranes[1].LUF6096 (10 μM; pretreated for 15 min) significantly and dramatically enhances the intrinsic activity of Cl-IB-MECA for the inhibition of the forskolin-stimulated cAMP production in CHO cells[1].
LUF6096 (twice i.v. bolus for 0.5 mg/kg or single i.v. bolus for 1 mg/kg) protects against myocardial ischemia/reperfusion injury in dogs[1].
参考文献:
[1]. Heitman LH, et, al. A series of 2,4-disubstituted quinolines as a new class of allosteric enhancers of the adenosine A3 receptor. J Med Chem. 2009 Feb 26;52(4):926-31.
[2]. Du L, et, al. Protection from myocardial ischemia/reperfusion injury by a positive allosteric modulator of the A? adenosine receptor. J Pharmacol Exp Ther. 2012 Jan;340(1):210-7.
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