Smith S M, Hughes D
MRC Neurochemical Pathology Unit, Newcastle General Hospital, U.K.
Brain Res. 1989 Jul 31;493(2):366-7. doi: 10.1016/0006-8993(89)91172-4.
Buspirone is an anxiolytic drug with an unknown mechanism of action. We have addressed the proposal that its therapeutic effect is due to a metabolite, 1-(2-pyrimidinyl)-piperazine (1-PP), increasing the open probability of gamma-aminobutyric acid (GABA)-activated channels. By making whole-cell recordings from cultured spinal neurones we demonstrated that 1-PP, in contrast to flurazepam, actually antagonizes GABA- and glycine-activated currents. These observations are inconsistent with this proposed mechanism of action for buspirone.
丁螺环酮是一种作用机制不明的抗焦虑药物。我们研究了这样一种观点，即其治疗效果归因于一种代谢产物1-(2-嘧啶基)-哌嗪（1-PP）增加了γ-氨基丁酸（GABA）激活通道的开放概率。通过对培养的脊髓神经元进行全细胞记录，我们发现与氟西泮相反，1-PP实际上拮抗GABA和甘氨酸激活的电流。这些观察结果与丁螺环酮这种提出的作用机制不一致。
