A positive allosteric modulator of adenosine A1 receptors
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
1.Aurelio, L., Figler, H., Flynn, B.L., et al.5-Substituted 2-aminothiophenes as A1 adenosine receptor allosteric enhancersBioorg. Med. Chem.16(3)1319-1327(2008) 2.Imlach, W.L., Bhola, R.F., May, L.T., et al.A positive allosteric modulator of the adenosine A1 receptor selectively inhibits primary afferent synaptic transmission in a neuropathic pain modelMol. Pharm.88(3)460-468(2015)
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