VCP 171
Chemical Name: [2-Amino-4-[3-(trifluoromethyl)phenyl]-3-thienyl]phenylmethanone
Purity: ≥98%
Biological Activity
VCP 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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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.
Mol.Pharmacol., 2015;88:460 -
5-Substituted 2-aminothiophenes as A1 adenosine receptor allosteric enhancers.
Aurelio et al.
Bioorg.Med.Chem., 2008;16:1319 -
Role of the second extracellular loop of the adenosine A1 receptor on allosteric modulator binding, signaling, and cooperativity.
Christopoulos et al.
Mol.Pharmacol., 2016;90:715
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