"The function of ATP-activated P2X3 receptors involved in pain sensation is modulated by desensitization, a phenomenon poorly understood. The present study used patch-clamp recording from cultured rat or mouse sensory neurons and kinetic modeling to clarify the properties of P2X3 receptor desensitization. ... Desensitization properties were well accounted for by a cyclic model in which receptors could be desensitized from either open or closed states. Recovery was assumed to be a multistate process with distinct kinetics dependent on the agonist-dependent dissociation rate from desensitized receptors. ... By using subthreshold concentrations of an HAD (high-affinity desensitization)-potent agonist, it might be possible to generate sustained inhibition of P2X3 receptors for controlling chronic pain."
Model Type: Channel/Receptor
Receptors: Sensory Receptors
Model Concept(s): Ion Channel Kinetics; Nociception
Simulation Environment: Pascal/Delphi
Implementer(s): Skorinkin, Andrei [askorink at yandex.ru]
References:
Sokolova E et al. (2006). Experimental and modeling studies of desensitization of P2X3 receptors. Molecular pharmacology. 70 [PubMed]