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4-甲基苄胺刺激食物摄入,并抵消苯丙胺作用于脑震颤样Kv1.1通道所产生的食欲减退效应。

4-methyl benzylamine stimulates food consumption and counteracts the hypophagic effects of amphetamine acting on brain Shaker-like Kv1.1 channels.

作者信息

Pirisino Renato, Galeotti Nicoletta, Livi Silvia, Raimondi Laura, Ghelardini Carla

机构信息

Department of Preclinical and Clinical Pharmacology, University of Florence, Viale Pieraccini 6, Florence 50134, Italy.

出版信息

Br J Pharmacol. 2006 Jan;147(2):218-24. doi: 10.1038/sj.bjp.0706465.

Abstract

1.--4-methyl benzylamine (4-MBZ; 28 microg, 231 nmol) elicits a hyperphagic response in starved mice in contrast to the hypophagia induced by the parent compound benzylamine (BZ; 33 microg, 231 nmol) or by amphetamine (AMPH, 2 mug). 2.--In mice starved for only 4 h, and therefore with little stimulation to eat, the maximal increase in food consumption induced by intracerebroventricular (i.c.v.)-injected 4-MBZ was 190% over that of the controls (ED(50) 8.3+/-2.7 microg mouse(-1); 68+/-22 nmol mouse(-1)), whereas after i.p. administration, these values were 160% and approximately 129 mg kg(-1), respectively. 3.--The hyperphagic effect of 4-MBZ was reduced by more than 60% in mice pretreated with antisense oligodeoxyribonucleotide (aODN(1)) previously found to selectively inhibit (over 50%) the expression of Shaker-like Kv1.1 channels. 4.--In mice highly stimulated to eat after 12-h fasting, 4-MBZ (28 microg) significantly reduced (to about 70%) the hypophagic response by AMPH (2 microg) or BZ (33 microg). Conversely, these two compounds reduced (respectively, by 69 and 44%) the hyperphagic response of 4-MBZ in 4-h fasting mice. 5.--4-MBZ (28 microg) also reduced the hypermotility and the stimulation of inspection activity elicited by AMPH in mice and the release of DA stimulated by AMPH (2 microg) from the nucleus accumbens of rats. We hypothesize that 4-MBZ elicits hyperphagic effects probably by opening Shaker-like Kv1.1 subtypes in the brain, whereas AMPH and BZ are hypophagic by blocking these channels.

摘要
  1. 与母体化合物苄胺(BZ;33微克,231纳摩尔)或苯丙胺(AMPH,2微克)诱导的摄食减少相反,4-甲基苄胺(4-MBZ;28微克,231纳摩尔)在饥饿小鼠中引发贪食反应。2. 在仅饥饿4小时、因此进食刺激很小的小鼠中,脑室内(i.c.v.)注射4-MBZ诱导的食物消耗最大增加量比对照组高190%(半数有效剂量为8.3±2.7微克/小鼠;68±22纳摩尔/小鼠),而腹腔注射后,这些值分别为160%和约129毫克/千克。3. 用先前发现能选择性抑制(超过50%)类Shaker型Kv1.1通道表达的反义寡脱氧核糖核苷酸(aODN(1))预处理的小鼠,4-MBZ的贪食效应降低了60%以上。4. 在禁食12小时后受到强烈进食刺激的小鼠中,4-MBZ(28微克)显著降低(至约70%)AMPH(2微克)或BZ(33微克)诱导的摄食减少反应。相反,这两种化合物分别使4小时禁食小鼠中4-MBZ的贪食反应降低了69%和44%。5. 4-MBZ(28微克)还降低了小鼠中AMPH引起的运动亢进和探究活动刺激,以及大鼠伏隔核中AMPH(2微克)刺激的多巴胺释放。我们推测,4-MBZ可能通过打开脑中的类Shaker型Kv1.1亚型引发贪食效应,而AMPH和BZ则通过阻断这些通道导致摄食减少。

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