Honda F, Satoh Y, Shimomura K, Satoh H, Noguchi H, Uchida S, Kato R
Jpn J Pharmacol. 1977 Jun;27(3):397-411. doi: 10.1254/jjp.27.397.
Effects of sulpiride on the central nervous system were studied in catalepsy induction (I) and antagonism to gnawing behaviour (II) induced by apomorphine and methamphetamine in normal rats, and in antagonism to rotational behaviour (III) induced by apomorphine and methamphetamine in rats with substantia nigra unilaterally lesioned chronically by microinjection of 6-hydroxydopamine. Sulpiride was administered orally and intraventricularly, and the effects of sulpiride were compared to those of haloperidol and chlorpromazine administered through the same routes. In oral administration, sulpiride was almost inactive in (I), and was several hundreds to a thousand times less potent than haloperidol in (II) and (III), while chlorpromazine was 20 to 150 times stronger than sulpiride. In intraventricular administration, sulpiride was almost equipotent to haloperidol in (I), and was equally effective to or 2 to 3 times more effective than halopridol in (III), although several times less in all respects. These findings suggest that sulpiride is essentially a potent inhibitory substance on dopamine receptors in the central nervous system and the rather weak central effects of peripherally given sulpiride are due to poor penetration through the blood brain barrier.
在正常大鼠中，研究了舒必利对阿扑吗啡和甲基苯丙胺诱导的僵住症（I）以及对啃咬行为的拮抗作用（II）的中枢神经系统效应；在通过微量注射6-羟基多巴胺单侧慢性损伤黑质的大鼠中，研究了舒必利对阿扑吗啡和甲基苯丙胺诱导的旋转行为的拮抗作用（III）。舒必利通过口服和脑室内给药，并将舒必利的效应与通过相同途径给药的氟哌啶醇和氯丙嗪的效应进行比较。口服给药时，舒必利在（I）中几乎无活性，在（II）和（III）中其效力比氟哌啶醇低数百至一千倍，而氯丙嗪比舒必利强20至150倍。脑室内给药时，舒必利在（I）中与氟哌啶醇几乎等效，在（III）中与氟哌啶醇同样有效或比其有效2至3倍，尽管在各方面都低几倍。这些发现表明，舒必利本质上是一种对中枢神经系统多巴胺受体有强效抑制作用的物质，外周给予的舒必利中枢效应较弱是由于其透过血脑屏障的能力较差。
