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首页> 外文期刊>Life sciences >CHRONIC IMIPRAMINE TREATMENT DOWNREGULATES IR1-IMIDAZOLINE RECEPTORS IN RAT BRAINSTEM
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CHRONIC IMIPRAMINE TREATMENT DOWNREGULATES IR1-IMIDAZOLINE RECEPTORS IN RAT BRAINSTEM

机译：慢性伊马汀治疗下调大鼠脑干中的IR1-咪唑啉受体

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One subtype of imidazoline receptors (IR1) is similar to alpha(2)-adrenoceptors (alpha(2)AR) based on their high affinity for clonidine and related imidazoline compounds. On the other hand, IR1 possess low affinity for norepinephrine (NE) and other catecholamines. Imidazoline receptors have also been found to be over-expressed in plasma membranes from platelets and brain tissues of depressed patients. Over-expression of IR1 in platelet membranes of depressed patients became normalized after various antidepressant treatments to the patients. Herein, the prototypic antidepressant imipramine (IMI), has been studied in regard to its treatment effects on [I-125]p-iodoclonidine binding to both alpha(2)AR and IR1 in rat brainstem membranes. No effects of chronic IMI treatment were found on brainstem alpha(2)AR binding sites (B-max and/or K-D parameters unchanged) after 25 days of daily injections (i.p. IMI 20 mg/kg/day). However, IMI induced a decrease in the density (B-max, measured under NE mask) of brainstem IR1 sites, with no change in K-D. Downregulation of IR1 sites was dose-dependent (minimal effective dose of i.p. IMI was 10 mg/kg/day) and time-dependent (> 16 days of treatment). These results implicate brainstem IR1 in the chronic effects of antidepressants. [References: 36]
机译：一种亚型的咪唑啉受体（IR1）与α（2）-肾上腺素能受体（alpha（2）AR）基于对可乐定和相关咪唑啉化合物的高度亲和力而相似。另一方面，IR1对去甲肾上腺素（NE）和其他儿茶酚胺的亲和力很低。还发现在抑郁症患者的血小板和脑组织的质膜中过表达咪唑啉受体。在对患者进行各种抗抑郁治疗后，抑郁患者的血小板膜中IR1的过度表达已恢复正常。在本文中，已研究了原型抗抑郁药丙咪嗪（IMI）对大鼠脑干膜中与[I-125] p-iodoclonidine结合α（2）AR和IR1的治疗作用。每天注射25天（i.p. IMI 20 mg / kg / day）后，未发现慢性IMI治疗对脑干alpha（2）AR结合位点（B-max和/或K-D参数保持不变）没有影响。但是，IMI引起脑干IR1位点密度的降低（B-max，在NE掩模下测量），而K-D不变。 IR1位点的下调取决于剂量（I.p. IMI的最小有效剂量为10 mg / kg /天）和取决于时间（治疗大于16天）。这些结果暗示脑干IR1参与抗抑郁药的慢性作用。 [参考：36]

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