Tam S Y, Roth R H
Department of Pharmacology, Yale University School of Medicine, New Haven, Connecticut.
J Pharmacol Exp Ther. 1990 Mar;252(3):989-96.
The benzodiazepine (BZ) recognition sites on the gamma-aminobutyric acid receptor/chloride ionophore complex have been suggested to be involved in the modulation of mesoprefrontal dopamine (DA) neurons. We have examined further the effects of different classes of BZ receptor ligands on DA metabolism in the prefrontal cortex. The anxiogenic inverse agonist FG 7142 elevated selectively 3,4-dihydroxyphenylacetic acid (DOPAC) levels and DO-PAC/DA ratio in the prefrontal cortex in a dose- and time-dependent manner. The activating effect was not, however, observed in any other mesocortical, mesolimbic or nigrostriatal DA terminal fields examined. Pretreatments with BZ agonists such as diazepam, flurazepam, lorazepam and CGS 9896 and BZ antagonists such as Ro15-1788 and CGS 8216 and barbiturates such as pentobarbital, significantly antagonized the beta-carboline-induced elevation of prefrontal DOPAC levels. Furthermore, a significant correlation was found between the pharmacological profile of different BZ receptor ligands on prefrontal DA metabolism and their profiles in behavioral, electrophysiological and receptor binding studies. Agonists increased DA levels and consequently decreased DOPAC/DA ratio in the prefrontal cortex. Inverse agonists, on the other hand, significantly elevated prefrontal DOPAC levels and DOPAC/DA ratio in a dose-dependent manner. Antagonists such as Ro15-1788 and CGS 8216, at low doses, did not alter mesoprefrontal DA metabolism, but at higher doses did elevate DOPAC/DA ratio in the prefrontal cortex.(ABSTRACT TRUNCATED AT 250 WORDS)
γ-氨基丁酸受体/氯离子载体复合物上的苯二氮䓬(BZ)识别位点被认为参与中前额叶多巴胺(DA)神经元的调节。我们进一步研究了不同类别的BZ受体配体对前额叶皮质中DA代谢的影响。致焦虑反向激动剂FG 7142以前额叶皮质中3,4-二羟基苯乙酸(DOPAC)水平和DOPAC/DA比值选择性升高,且呈剂量和时间依赖性。然而,在所检测的任何其他中皮质、中边缘或黑质纹状体DA终末区域均未观察到这种激活作用。用BZ激动剂如地西泮、氟西泮、劳拉西泮和CGS 9896、BZ拮抗剂如Ro15-1788和CGS 8216以及巴比妥类药物如戊巴比妥预处理,可显著拮抗β-咔啉诱导的前额叶DOPAC水平升高。此外,不同BZ受体配体在前额叶DA代谢方面的药理学特征与其在行为、电生理和受体结合研究中的特征之间存在显著相关性。激动剂可增加前额叶皮质中的DA水平,从而降低DOPAC/DA比值。另一方面,反向激动剂以剂量依赖性方式显著升高前额叶DOPAC水平和DOPAC/DA比值。低剂量的Ro15-1788和CGS 8216等拮抗剂不会改变中前额叶DA代谢,但高剂量时会升高前额叶皮质中的DOPAC/DA比值。(摘要截选至250字)