Inhibitory Effects of Pentamidine on N-Methyl-D-aspartate (NMDA) Receptor/Channels in the Rat Brain

概要

論文の詳細を見る
Effects of pentamidine, a therapeutic drug for Pneumocystis carinii pneumonia (PCP) in acquired immunodeficiency syndrome (AIDS), on specific bindings of [^3H] (+)-5-methyl-10,11-dihydro-5H-dibenzo [a, d] cyclohepten-5,11-imine maleate (MK-801) and [^3H] nitrendipine were investigated in crude synaptic membranes (CSM) of rat brain. Pentamidine inhibited [^3H] MK-801 binding but did not change [^3H] nitrendipine binding, althouth neither binding was inhibited by 3'-azido-2', 3'-dideoxycytidine (inhibitors for reverse transcriptase of HIV-1), or FK-506 or cyclosporin A (immunosuppressants). In Triton X-100-treated CSM (post-synaptic density-rich fractions), the inhibitory effect of pentamidine on [^3H] MK-801 binding was partially prevented by addition of spermine and NMDA plus glycine (Gly). Electrophysiological experiments showed that pentamidine also inhibited Ca^<2+>-current evoked by NMDA plus Gly in Xenopus oocytes injected with rat brain mRNA. These results suggest that pentamidine is a potent inhibitor for NMDA receptor/channels.
公益社団法人日本薬学会の論文
1995-02-15