Sesack S R, Bunney B S
Department of Pharmacology, Yale University School of Medicine, New Haven, Connecticut.
J Pharmacol Exp Ther. 1989 Mar;248(3):1323-33.
The pharmacological profile of the receptor mediating inhibitory effects of dopamine (DA) in the rat medial prefrontal cortex (PFC) was characterized using extracellular single unit recording and microiontophoretic techniques. Iontophoretic application of DA inhibited 65% of spontaneously active cells in the deep layers of the PFC, while producing little effect on cells in superficial laminae. The D2 selective antagonist, sulpiride, specifically attenuated DA-induced inhibition of deep layer PFC neurons, without blocking the inhibitory effects of gamma-aminobutyric acid (GABA) or serotonin (5-HT). Surprisingly, sulpiride antagonism did not appear to be stereospecific, as both its (-)- and (+)-isomers proved equally effective at blocking the inhibitory effects of DA. In contrast to sulpiride, the D1 selective antagonist, SCH23390, was much less effective at attenuating inhibitory responses to DA. The effects of selective agonists also were examined on DA-sensitive PFC neurons. The D2 selective agonist, LY171555, and the D1 selective agonist, SKF38393, produced inhibitory effects on a small number of DA-sensitive PFC neurons. However, the majority of cells tested were inhibited only by DA and not by LY171555 or SKF38393. In addition, coiontophoresis of LY171555 and SKF38393. In addition, coiontophoresis of LY171555 and SKF38393 failed to inhibit the majority of DA-sensitive PFC cells tested. LY171555, but not SKF38393, significantly attenuated DA-induced inhibition when applied simultaneously, suggesting that the D2 selective agonist might possess partial agonist/weak antagonist activity at this receptor. These results indicate that the receptor mediating the inhibitory effects of DA in the medial PFC has the pharmacological characteristics of a D2 subtype. However, this receptor may not be identical to D2 sites in other brain regions.
运用细胞外单单位记录和微离子电泳技术,对介导多巴胺(DA)在大鼠内侧前额叶皮质(PFC)中抑制作用的受体的药理学特性进行了表征。离子电泳施加DA可抑制PFC深层中65%的自发活动细胞,而对浅层细胞的影响很小。D2选择性拮抗剂舒必利特异性减弱了DA对PFC深层神经元的诱导抑制作用,而不阻断γ-氨基丁酸(GABA)或5-羟色胺(5-HT)的抑制作用。令人惊讶的是,舒必利的拮抗作用似乎不是立体特异性的,因为其(-)-和(+)-异构体在阻断DA的抑制作用方面同样有效。与舒必利相反,D1选择性拮抗剂SCH23390在减弱对DA的抑制反应方面效果要差得多。还研究了选择性激动剂对DA敏感的PFC神经元的作用。D2选择性激动剂LY171555和D1选择性激动剂SKF38393对少数DA敏感的PFC神经元产生了抑制作用。然而,大多数测试细胞仅被DA抑制,而未被LY171555或SKF38393抑制。此外,LY171555和SKF38393的联合离子电泳未能抑制大多数测试的DA敏感PFC细胞。当同时应用时,LY171555而非SKF38393显著减弱了DA诱导的抑制作用,这表明D2选择性激动剂在该受体上可能具有部分激动剂/弱拮抗剂活性。这些结果表明,介导DA在内侧PFC中抑制作用的受体具有D2亚型的药理学特征。然而,该受体可能与其他脑区的D2位点不同。