EFFECTS OF ANTIDEPRESSANTS ON THE INWARD CURRENT MEDIATED BY 5-HT3 RECEPTORS IN RAT NODOSE GANGLION NEURONS
EFFECTS OF ANTIDEPRESSANTS ON THE INWARD CURRENT MEDIATED BY 5-HT3 RECEPTORS IN RAT NODOSE GANGLION NEURONS
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DOI：
10.1111/j.1476-5381.1994.tb13140.x
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发表时间：
1994-07-01
影响因子：
7.3
通讯作者：
FAN, P
中科院分区：
文献类型：
--
作者：
FAN, P
1 在大鼠结节神经元中研究了三种不同类别的抗抑郁药：丙咪嗪（三环）、氟西汀（选择性 5-羟色胺 (5-HT) 摄取抑制剂）、苯乙肼和异丙烟肼（单胺氧化酶 (MAO) 抑制剂）对 5-HT3 受体介导的内向电流的影响。全细胞膜片钳技术用于记录 5-HT 电流。2 所有测试的抗抑郁药均抑制 5-HT 峰值电流。抑制逐渐达到稳定水平，并且当去除抗抑郁药物时恢复不完全。丙咪嗪、氟西汀和苯乙肼的IC50值分别为0.54μM、1.3μM和4.2μM。相应的 Hill 系数分别为 0.9、0.87 和 0.92.3。所检测的抗抑郁药增加了 5-HT 电流脱敏率。丙咪嗪、氟西汀和苯乙肼对脱敏时间常数降低的IC50值分别为0.11μM、0.18μM和2.4μM。相应的 Hill 系数分别为 0.9、1.14 和 1.06.4 细胞内应用蛋白激酶抑制剂 H-7 (100 μM)、GDP-β-S (2 mM) 和钙螯合剂 BAPTA (20 mM) 不会影响 5-HT 电流以及抗抑郁药对 5-HT 电流的作用。 5 这些结果表明 5-HT3 受体是治疗用途的作用位点。抗抑郁药。目前的观察结果也有助于解释疼痛诊所中抗抑郁药的镇痛作用。
1 Effects of three different categories of antidepressants, imipramine (tricyclic), fluoxetine (selective 5-hydroxytryptamine (5-HT) uptake inhibitor), phenelzine and iproniazid (monoamine oxidase (MAO) inhibitor) on the inward current mediated by 5-HT3 receptors were investigated in rat nodose ganglion neurones. The whole-cell patch-clamp technique was used for recording the 5-HT current.2 All the antidepressants tested inhibited the peak 5-HT current. The inhibition gradually reached a steady level and the recovery was incomplete when antidepressants were removed. IC50 values for imipramine, fluoxetine and phenelzine were 0.54 mu M, 1.3 mu M and 4.2 mu M respectively. The correspondent Hill coefficients were 0.9, 0.87 and 0.92.3 The antidepressants examined increased the rate of 5-HT current desensitization. IC50 values for imipramine, fluoxetine and phenelzine on the decrease in desensitization time constant were 0.11 mu M, 0.18 mu M and 2.4 mu M respectively. The correspondent Hill coefficients were 0.9, 1.14 and 1.06.4 Intracellular applications of the protein kinase inhibitor, H-7 (100 mu M), GDP-beta-S (2 mM) and the calcium chelator BAPTA (20 mM) did not affect the 5-HT current and the actions of antidepressants on 5-HT current.5 These results suggest that the 5-HT3 receptor is an acting site for the therapeutic use of antidepressants. The present observation is also helpful in explaining the analgesic effect of antidepressants seen in pain clinics.