Klimek V, Nowak G, Zak J, Maj J
Institute of Pharmacology, Polish Academy of Sciences, Krakow, Poland.
Neurosci Lett. 1990 Jan 1;108(1-2):189-94. doi: 10.1016/0304-3940(90)90729-s.
The binding of [3H]prazosin to alpha 1-adrenoreceptors, as well as of [3H]SCH 23390 (R(+)-8-chloro-2,3,4,5-tetrahydro-3-methyl-5-phenyl-1H-3-benzazepine-7-o l) to dopamine D1 receptors, and [3H]spiperone to D2 receptors was studied following repeated administration of the monoamine oxidase inhibitors (MAOI) brofaromine, moclobemide and deprenyl to rats. Scatchard analysis showed no change in the density (Bmax) and affinity (Kd) of [3H]prazosin sites, yet the ability of phenylephrine (an alpha 1-adrenoceptor agonist) to compete for [3H]antagonist binding sites was enhanced in the cerebral cortex after repeated brofaromine administration, as well as in the hippocampus of rats pretreated with moclobemide and deprenyl. The density and the binding affinity of dopaminergic D1 and D2 receptors were not affected by repeated treatment with all the MAOI used. The results seem to indicate that a small increase in the alpha 1-adrenoceptor agonist affinity occurs after repeated administration of MAOI.
在向大鼠反复给予单胺氧化酶抑制剂（MAOI）溴法罗明、吗氯贝胺和司来吉兰后，研究了[3H]哌唑嗪与α1 - 肾上腺素能受体的结合，以及[3H]SCH 23390（R(+)-8 - 氯 - 2,3,4,5 - 四氢 - 3 - 甲基 - 5 - 苯基 - 1H - 3 - 苯并氮杂卓 - 7 - 醇）与多巴胺D1受体的结合，还有[3H]螺哌隆与D2受体的结合。Scatchard分析表明，[3H]哌唑嗪位点的密度（Bmax）和亲和力（Kd）没有变化，然而，在反复给予溴法罗明后，以及在给予吗氯贝胺和司来吉兰预处理的大鼠海马中，去氧肾上腺素（一种α1 - 肾上腺素能受体激动剂）竞争[3H]拮抗剂结合位点的能力在大脑皮层中增强。所有使用的MAOI反复治疗均未影响多巴胺能D1和D2受体的密度和结合亲和力。结果似乎表明，反复给予MAOI后，α1 - 肾上腺素能受体激动剂的亲和力会有小幅增加。
