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首页> 外文期刊>Neurochemistry International: The International Journal for the Rapid Publication of Critical Reviews, Preliminary and Original Research Communications in Neurochemistry >Effect of chronic paroxetine treatment on 5-HT1B and 5-HT1D autoreceptors in rat dorsal raphe nucleus.
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Effect of chronic paroxetine treatment on 5-HT1B and 5-HT1D autoreceptors in rat dorsal raphe nucleus.

机译：慢性帕罗西汀治疗对大鼠背沟核中5-HT1B和5-HT1D自身受体的影响。

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摘要

This study reports the effect of chronic paroxetine (10 mg/kg p.o., 21 days) on 5-HT1B and 5-HT1D autoreceptors controlling stimulated 5-HT efflux in slices of rat dorsal raphe nucleus. Electrically evoked 5-HT (10 pulses, 200 Hz, 0.1 ms, 10 mA) was measured using fast cyclic voltammetry. 5-HT efflux was inhibited by CP 93129 (10 nM-10 microM) and by sumatriptan (1 nM-1 microM) agonists at 5-HT1B and 5-HT1D receptors, respectively. Chronic paroxetine did not, initially, appear to alter the sensitivity of the 5-HT1B autoreceptors to CP 93129. However, when constructed in the presence of WAY 100635 (10 nM) the selective and silent 5-HT1A antagonist, there was a significant (P < 0.001) rightward shift of the CP 93129 concentration-response curve in the paroxetine-treated rats but not in the controls, implying a desensitisation of the 5-HT1B autoreceptor by paroxetine. Chronic paroxetine did not affect the sumatriptan concentration-response curve, even with WAY 100635 present, implying that there was no (de)sensitisation of the 5-HT1D autoreceptor. These data suggest that chronic paroxetine treatment may desensitise 5-HT1B autoreceptors in the dorsal raphe nucleus but that this effect is unmasked only when the dominant 5-HT1A autoreceptor control is antagonised.
机译：这项研究报告了慢性帕罗西汀（10 mg / kg p.o.，21天）对控制大鼠背沟核切片中刺激的5-HT外排的5-HT1B和5-HT1D自体受体的影响。使用快速循环伏安法测量电诱发的5-HT（10个脉冲，200 Hz，0.1 ms，10 mA）。 CP 93129（10 nM-10 microM）和舒马曲坦（1 nM-1 microM）激动剂分别在5-HT1B和5-HT1D受体处抑制5-HT外排。最初，慢性帕罗西汀似乎并未改变5-HT1B自体受体对CP 93129的敏感性。但是，当在WAY 100635（10 nM）存在的情况下构建选择性且沉默的5-HT1A拮抗剂时，存在显着（ P <0.001）在帕罗西汀治疗的大鼠中CP 93129浓度-反应曲线向右移动，但在对照中则没有，这意味着帕罗西汀会使5-HT1B自体受体脱敏。即使存在WAY 100635，慢性帕罗西汀也不会影响舒马曲坦的浓度-反应曲线，这表明5-HT1D自身受体没有（脱敏）作用。这些数据表明，慢性帕罗西汀治疗可能会使背睑核中的5-HT1B自体受体脱敏，但只有在显性的5-HT1A自体受体拮抗剂被拮抗的情况下，这种作用才得以掩盖。

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