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VCP171 is a positive allosteric modulator of adenosine A1 receptors (EC50 = 15.8 μM in a kinetic assay measuring agonist dissociation).1. It reduces AMPA receptor-mediated evoked excitatory postsynaptic currents (eEPSCs) in lamina I and lamina II neurons in a rat model of neuropathic pain (EC50s = 1.995 and 0.251 μM, respectively) to a greater extent than in sham control animals (EC50s = 2.512 and 0.631 μM, respectively).2
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2. A positive allosteric modulator of the adenosine A1 receptor selectively inhibits primary afferent synaptic transmission in a neuropathic pain model. Mol. Pharm. 88(3), 460-468 (2015).