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MIPS521 is an adenosine A1 receptor positive allosteric modulator.1 It binds to adenosine A1 receptors (Kb = 11 µM) and enhances adenosine-induced inhibition of forskolin-induced cAMP production in CHO cells expressing recombinant human adenosine A1 receptors when used at concentrations ranging from 0.3 to 30 µM. In vivo, MIPS521 (10 and 30 µg/animal) increases the mechanical paw withdrawal threshold in a rat model of neuropathic pain induced by partial sciatic nerve ligation.
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1. Positive allosteric mechanisms of adenosine A1 receptor-