LUF6096

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 In Vitro LUF6096 (10 μM; 30-120 min) decreases the dissociation rate of 125 I-AB-MECA from the A 3 receptor by 2.5 times in CHO cell membranes. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Adult mongrel dogs (15-25 kg) were subjected left anterior descending (LAD) coronary artery occlusion and reperfusion Dosage: Twice i.v. bolus for 0.5 mg/kg or single i.v. bolus for 1 mg/kg Administration: I.v. bolus Result: Produced a marked reduction in infarct size (∼50% reduction) compared with vehicle-treated dogs. IC50& Target:adenosine A3 receptor

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