Figure 1.
A model for the role of sensitization of nociceptive dorsal horn neuron in pain hypersensitivity. Left; under basal conditions NMDAR activity is suppressed by partial blockade of the channel by Mg2+ and by the activity of the protein tyrosine phosphatase, STEP, and the kinase, Csk. KAIR, kainate receptor. Middle; nociceptive input increases NMDAR-mediated currents by 1) relief of Mg2+ inhibition, 2) by activation of Src (Src*) via the actions of PTPa and activated CAKβ (CAKβ-P) which overcomes the suppression by STEP, and 3) by sensitizing the NMDARs to raised intracellular [Na+]. Right; upregulation of NMDAR function allows a large boost in entry of Ca2+, which binds to calmodulin (CaM) causing activation of CaMKII, not illustrated. The enhancement of glutamatergic transmission is ultimately expressed through increased numbers of AMPA/KAIRs in the postsynaptic membrane and/or enhanced AMPA/KAIR activity.