首页> 外文期刊>European Journal of Pharmacology: An International Journal >Region-dependent effects of acute and chronic tranylcypromine in vivo on (3H)2-BFI binding to brain imidazoline I(2) sites.
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Region-dependent effects of acute and chronic tranylcypromine in vivo on (3H)2-BFI binding to brain imidazoline I(2) sites.

机译:急性和慢性反式环丙胺在体内对(3H)2-BFI绑定到脑咪唑啉I(2)网站的区域依赖性影响。

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摘要

An imidazoline I(2) site has been localised to monoamine oxidase. However, in vitro studies of the effect of monoamine oxidase inhibitors on imidazoline I(2)-site radioligand binding have produced conflicting findings. Using the technique of autoradiography, we examined the effect of in vivo administration of the irreversible monoamine oxidase inhibitor tranylcypromine on binding of the imidazoline I(2) site-specific ligand [3H]2-(-2-benzofuranyl)-2-imidazoline ([3H]2-BFI) in four rat brain nuclei which are known to possess a high density of imidazoline I(2) sites, together with cerebral cortex and cerebellum which show weaker binding. A single acute pre-treatment with tranylcypromine significantly increased imidazoline I(2) site-specific binding in four regions: arcuate nucleus, interpeduncular nucleus, pineal gland and area postrema, but effects in cortical areas and cerebellum were not significant. The extent of the increase was proportional to the control binding in each region. In contrast, five daily treatments with the same dose of tranylcypromine significantly reduced [3H]2-BFI binding in these same areas. The potential role of monoamine oxidase isoforms in these changes is discussed.
机译:咪唑啉I(2)网站已被定位为单胺氧化酶。但是,单胺氧化酶抑制剂对咪唑啉I(2)-位放射性配体结合的影响的体外研究产生了矛盾的发现。使用放射自显影技术,我们检查了体内给予不可逆单胺氧化酶抑制剂tranylcypromine对咪唑啉I(2)位点特异性配体[3H] 2-(-2-苯并呋喃基)-2-咪唑啉( [3H] 2-BFI)在四个大鼠脑核中,已知它们具有高密度的咪唑啉I(2)位点,以及显示较弱结合的大脑皮层和小脑。单个急性预处理用tranylcypromine可以显着提高咪唑啉I(2)在四个区域的特定部位的结合:弓形核,椎弓根间核,松果体和术后区域,但对皮质区域和小脑的影响并不明显。增加的程度与每个区域中的对照结合成比例。相比之下,每日五次使用相同剂量的反式环丙胺治疗可显着降低这些区域中[3H] 2-BFI的结合。讨论了单胺氧化酶同工型在这些变化中的潜在作用。

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