Moriuchi K, Imazu Y, Yoneda H
Department of Neuropsychiatry, Osaka Medical College, Japan.
Neurochem Res. 1995 Jan;20(1):95-9. doi: 10.1007/BF00995158.
Sultopride and sulpiride are both chemically similar benzamide derivatives and selective antagonists of dopamine D2 receptors. However, these drugs differ in clinical properties. We compared the effects of sultopride and sulpiride on dopamine turnover in rats following the administration of these drugs alone or in combination with apomorphine. The administration of sultopride or sulpiride markedly accelerated dopamine turnover in the rat brain. The increase in the level of dopamine metabolites in the striatum was more marked in the sultopride-treated rats. Sulpiride affected the limbic dopamine receptors preferentially, whereas sultopride affected the striatal and the limbic dopamine receptors equally. A low dose of apomorphine induced a reduction in the concentration of dopamine metabolites in the striatum and the nucleus accumbens by approximately 55%, but not in the medial prefrontal cortex. Sultopride was more effective in preventing an apomorphine-induced reduction in dopamine metabolite levels. These results from rat experiments would model the pharmacological differences observed between sultopride and sulpiride in clinical use.
舒托必利和舒必利都是化学结构相似的苯甲酰胺衍生物，是多巴胺D2受体的选择性拮抗剂。然而，这些药物在临床特性上有所不同。我们比较了舒托必利和舒必利单独给药或与阿扑吗啡联合给药后对大鼠多巴胺代谢的影响。舒托必利或舒必利的给药显著加速了大鼠脑内的多巴胺代谢。舒托必利治疗组大鼠纹状体中多巴胺代谢产物水平的升高更为明显。舒必利优先作用于边缘系统的多巴胺受体，而舒托必利对纹状体和边缘系统的多巴胺受体作用相当。低剂量的阿扑吗啡使纹状体和伏隔核中多巴胺代谢产物的浓度降低了约55%，但内侧前额叶皮质中未降低。舒托必利在预防阿扑吗啡引起的多巴胺代谢产物水平降低方面更有效。大鼠实验的这些结果将模拟舒托必利和舒必利在临床应用中观察到的药理学差异。
