Bischoff S, Bittiger H, Delini-Stula A, Ortmann R
Eur J Pharmacol. 1982 Apr 23;79(3-4):225-32. doi: 10.1016/0014-2999(82)90628-8.
Effects of the substituted benzamide, and of oxiperomide on DA receptors and on Da-related behaviors were the object of the study. The benzamides were practically inactive on DA-sensitive adenylate cyclase and on in vitro [3H] spiperone binding (in the absence of sodium ions). However, all of them inhibited in vivo [3H] spiperone binding in various rat brain regions; this in vivo effect was especially apparent in hippocampus and septum. In frontal cortex, the benzamides (with the exception of metoclopramide) produced only a partial inhibition of [3H] spiperone binding. Such inhibition also occurred in the striatum with sulpiride and tiapride. The results suggest that substituted benzamides are DA antagonists due to their ability to inhibit in vivo [3H] spiperone binding. The lack of agreement between in vivo and in vitro tests is also discussed.
本研究旨在探讨取代苯甲酰胺及奥氮平对多巴胺(DA)受体和与DA相关行为的影响。这些苯甲酰胺类药物对DA敏感的腺苷酸环化酶及体外[3H]螺哌隆结合(在无钠离子存在时)几乎无活性。然而,它们均能抑制大鼠不同脑区的体内[3H]螺哌隆结合;这种体内效应在海马和隔区尤为明显。在额叶皮质,苯甲酰胺类药物(除甲氧氯普胺外)仅对[3H]螺哌隆结合产生部分抑制。舒必利和替加色罗在纹状体中也出现了这种抑制作用。结果表明,取代苯甲酰胺类药物因其能够抑制体内[3H]螺哌隆结合而属于DA拮抗剂。文中还讨论了体内和体外试验结果不一致的情况。