Abstract
Although it has been reported that desipramine affects ion-channel activity of NMDA receptor/ion-channel complexes, the binding sites remain unclear. To identify the binding site, influences of desipramine on NMDA-induced current were examined in Xenopus oocytes injected with rat brain RNA and compared with those of blockers, MK-801, Zn 2+ and Mg 2+. Application of 100 μM desipramine irreversibly inhibited NMDA-induced inward current as well as 1 μM MK-801. Mg 2+ and Zn 2+ showed a reversible inhibition. Pretreatment with Mg 2+ or Zn 2+ abolished the irreversible inhibition of desipramine. In contrast, the irreversible inhibition of desipramine was still observed after application of Mg 2+ and Zn 2+. These results suggest that Mg 2+/Zn 2+ and desipramine bind on different sites from each other and affect the cation permeability via different mechanisms. Regarding inhibitory effects of other antidepressant drugs, imipramine and setiptiline were found to markedly inhibit NMDA current, while maprotiline, amitriptyline and lofepramine slightly inhibited the current. Mianserin, a potent antagonist of 5-HT 1c receptors, however, had no influence.
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