Chemical Name: [2-Amino-4-[3-(trifluoromethyl)phenyl]-3-thienyl]phenylmethanone
Biological ActivityVCP 171 is an adenosine A1 receptor positive allosteric modulator (PAM) (pKB = 5.65, binding cooperativity with NECA 0.68). In absence of orthosteric agonist, VCP171 behaves as an allosteric partial agonist, inhibiting cAMP activity. Inhibits AMPA receptor-mediated evoked excitatory postsynaptic current (eEPSC) amplitude in lamina I and II neurons in a rat partial nerve-injury model of neuropathic pain.
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A positive allosteric modulator of the adenosine A1 receptor selectively inhibits primary afferent synaptic transmission in a neuropathic pain model.
Imlach et al.
5-Substituted 2-aminothiophenes as A1 adenosine receptor allosteric enhancers.
Aurelio et al.
Role of the second extracellular loop of the adenosine A1 receptor on allosteric modulator binding, signaling, and cooperativity.
Christopoulos et al.
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