"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
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
Sokolova E, Skorinkin A, Moiseev I, Agrachev A, Nistri A, Giniatullin R (2006) Experimental and modeling studies of desensitization of P2X3 receptors. Mol Pharmacol 70:373-82 [PubMed]