Meos A A, Kudrin V S, Raevskiĭ K S
Biull Eksp Biol Med. 1984 Sep;98(9):305-8.
An in vitro study was made of the influence of the atypical neuroleptics sulpiride and carbidine on the activity of synaptosomal tyrosine hydroxylase (TH) of the rat brain striatum. Dopamine was applied as an inhibitor of tyrosine hydroxylation (10(-6) M), dopamine uptake was blocked by nomifensine (10(-5) M). The experiments were performed in two versions: in a medium containing common (5 mM) and depolarizing concentration of potassium ions. In both the cases sulpiride did not exert any noticeable effect on TH activity but significantly lowered the inhibitory action of dopamine. In a medium containing 30 mM potassium, carbidise inhibited the rate of TH hydroxylation and enhanced the inhibitory action of dopamine on TH activity under blockade of its uptake by nomifensine. It is assumed that the mechanisms of the action of carbidine and sulpiride are different.
进行了一项体外研究,以探讨非典型抗精神病药物舒必利和卡比多巴对大鼠脑纹状体突触体酪氨酸羟化酶(TH)活性的影响。使用多巴胺作为酪氨酸羟化作用的抑制剂(10⁻⁶ M),用诺米芬辛(10⁻⁵ M)阻断多巴胺摄取。实验分两种情况进行:在含有普通(5 mM)钾离子浓度和去极化钾离子浓度的培养基中。在这两种情况下,舒必利对TH活性均未产生明显影响,但显著降低了多巴胺的抑制作用。在含有30 mM钾离子的培养基中,卡比多巴抑制了TH羟化速率,并在诺米芬辛阻断多巴胺摄取的情况下增强了多巴胺对TH活性的抑制作用。据推测,卡比多巴和舒必利的作用机制不同。