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用全细胞膜片箝技术在大鼠新鲜分离的背根神经节 (DRG)细胞上观察到baclofen对GABA和NMDA激活电流有调制作用。单独给予DRG细胞baclofen (1～ 10 0 μmol/L)未记录到可测的电流改变 ,但预加baclofen对GABA和NMDA激活电流具有明显的抑制作用 ,且呈剂量依赖性。 10 0 μmol/Lbaclofen对GABA和NMDA激活电流分别抑制(5 1.2± 10 .9) % (X±SE ,n=8,P <0 .0 1)和 (6 4 .1± 2 1.1) % (X±SE ,n=6 ,P <0 .0 1) ,此抑制作用是可逆的 ,可被GABAB 受体拮抗剂saclofen(10 0 μmol/L ) 所取消 (n =4 )。
Baclofen was observed to modulate GABA and NMDA activation currents in freshly isolated dorsal root ganglion (DRG) cells of rats using whole-cell patch clamp techniques. No measurable change in current was detected in baclofen (1-10 μmol / L) alone given DRG cells, but pretreatment with baclofen significantly inhibited GABA and NMDA activation currents in a dose-dependent manner. The inhibitory effect of 10 μmol / L baclofen on GABA and NMDA activation currents was (5 1.2 ± 10.9)% (X ± SE, n = 8, P <0.01) and (6.4 ± 2.1.1)% X ± SE, n = 6, P <0.01). The inhibitory effect was reversible and could be canceled by the GABAB receptor antagonist saclofen (100 μmol / L) (n = 4).