Maĭsov N I, Sandalov Iu G, Glebov R N, Raevskiĭ K S
Biull Eksp Biol Med. 1976 Jan;81(1):45-7.
The centrally acting drugs belonging to different groups--fluphenazine, trifluperidol, phthoracyzine, imipramine, diazepam, apomorphine, fentanyl, diphneylhydantoin, nonachlazine displayed in vitro an inhibitory effect on the uptake of gamma-aminobutyric acid by rat brain synaptosomes. A decrease in the activity of synaptosomal Na,K-ATPase was found in most cases. Drugs that failed to alter GABA uptake were as a rule found to be ineffective in relation to the enzyme activity (carbidine, morphine). GABA uptake was not affected by certain drugs inhibiting the Na,K-ATPase activity (azabuperon, tetrabenazine). It is supposed that the drugs used had at least two possible sites of action - Na,K-ATPase itself and hypothetic GABA transmembrane carrier.
属于不同组别的中枢作用药物——氟奋乃静、三氟哌多、甲硫达嗪、丙咪嗪、地西泮、阿扑吗啡、芬太尼、苯妥英、诺氯嗪,在体外对大鼠脑突触体摄取γ-氨基丁酸具有抑制作用。在大多数情况下,发现突触体钠钾-ATP酶的活性降低。通常发现未能改变γ-氨基丁酸摄取的药物对该酶活性无效(卡比多巴、吗啡)。某些抑制钠钾-ATP酶活性的药物(阿扎必利、丁苯那嗪)对γ-氨基丁酸摄取没有影响。据推测,所使用的药物至少有两个可能的作用位点——钠钾-ATP酶本身和假设的γ-氨基丁酸跨膜载体。