Stable, synthetic analogs of diadenosine tetraphosphate inhibit rat and human P2X3 receptors and inflammatory pain

Conclusions
Stable, synthetic Ap4A analogs (AppNHppA and AppCH2ppA) being weak partial agonist provoke potent high-affinity desensitization-mediated inhibition of homomeric P2X3Rs at low concentrations. Therefore, both analogs demonstrate clear potential as potent analgesic agents for use in the management of chronic pain associated with heightened P2X3R activation.

Source: Molecular Pain - March 28, 2016 Category: Molecular Biology Authors: Viatchenko-Karpinski, V., Novosolova, N., Ishchenko, Y., Azhar, M. A., Wright, M., Tsintsadze, V., Kamal, A., Burnashev, N., Miller, A. D., Voitenko, N., Giniatullin, R., Lozovaya, N. Tags: Original Article Source Type: research