Antonikov I M, Mel'nik V I, Glebov R N
Biull Eksp Biol Med. 1986 Dec;102(12):714-7.
The effects of trifluoperazine (TFP) on some membrane processes were studied in the isolated rat brain synaptic vesicles (SV). TFP (10(-5)-10(-4) M) was found to cause a sharp rise in the intensity of light scattering by SV suspension which was due both to an increased vesicle aggregation and to changes in the refraction index of the membrane. In addition, TFP blocked the ATP-dependent proton transport into the vesicles (K0.5 = 10(-6) M) with the concomitant stimulation of the ATPase activity which suggests an uncoupling effect caused by the permeation of this weak base through the membrane and subsequent protonation in an acid interior medium resulting in the elimination of a proton gradient. Thus, the neuroleptic drug--TFP has various effects on membrane processes which are apparently unrelated to its recognized role as a calmodulin antagonist.
研究了三氟拉嗪(TFP)对离体大鼠脑突触小泡(SV)某些膜过程的影响。发现TFP(10⁻⁵ - 10⁻⁴ M)会导致SV悬浮液的光散射强度急剧增加,这既归因于小泡聚集增加,也归因于膜折射率的变化。此外,TFP阻断了依赖ATP的质子向小泡内的转运(K0.5 = 10⁻⁶ M),同时刺激了ATP酶活性,这表明该弱碱透过膜渗透并在酸性内部介质中随后质子化,导致质子梯度消除,从而产生解偶联效应。因此,抗精神病药物TFP对膜过程有多种影响,这些影响显然与其作为钙调蛋白拮抗剂的公认作用无关。