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DPTN is an adenosine A3 receptor antagonist (Ki = 0.36 nM for the human receptor).1 It is selective for the adenosine A3 receptor over the adenosine A1 and A2A receptors (Kis = >666 and >826 nM, respectively). DPTN (10 mg/kg) prevents dye leakage in a rat model of plasma extravasation induced by the adenosine A3 receptor agonist IB-MECA (piclidenoson; Item No. 28445). It, alone and in combination with the synthetic glucocorticoid dexamethasone (Item No. 11015), inhibits airway hypersensitivity to acetylcholine in a rat model of allergen-induced asthma stimulated by ovalbumin inhalation when administered at a dose of 10 mg/kg.
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1. Synthesis and biological activities of 4-