利用有机阳离子[14C] - 胍的内流对N1E - 115神经母细胞瘤细胞的5 - HT3受体进行表征。
Characterization of 5-HT3 receptors of N1E-115 neuroblastoma cells by use of the influx of the organic cation [14C]-guanidinium.
作者信息
Bönisch H, Barann M, Graupner J, Göthert M
机构信息
Institut für Pharmakologie und Toxikologie, Universität Bonn, Germany.
出版信息
Br J Pharmacol. 1993 Feb;108(2):436-42. doi: 10.1111/j.1476-5381.1993.tb12822.x.
Abstract
- The 5-HT3 receptor-mediated cation influx into N1E-115 mouse neuroblastoma cells has been studied by the use of the organic cation [14C]-guanidinium. 2. 5-Hydroxytryptamine (5-HT, 30 microM) caused a time-dependent influx of [14C]-guanidinium which, in contrast to the influx elicited by veratridine (100 microM), was not inhibited by tetrodotoxin (TTX, 10 microM). The 5-HT-induced influx was potentiated by substance P and inhibited by ondansetron. 3. 5-HT and the selective 5-HT3 receptor agonists, m-chloro-phenylbiguanide, phenylbiguanide and 2-methyl-5-HT caused bell-shaped concentration-response curves; the rank order of potency was m-chloro-phenylbiguanide > 5-HT > phenylbiguanide = 2-methyl-5-HT. Among these agonists, 5-HT elicited the highest influx of [14C]-guanidinium. 5-Methoxytryptamine, an agonist at 5-HT4 receptors, showed no effect. 4. The [14C]-guanidinium influx induced by 100 microM 5-HT was not affected by methysergide (10 microM) and ketanserin (10 microM) but was inhibited by 5-HT3 receptor antagonists with the following rank order of potency: ICS 205-930 > ondansetron > MDL 72222 >> metoclopramide. 5. The 5-HT-induced [14C]-guanidinium influx was increased in the absence of Ca2+ and/or Na+ and by a reduction of the temperature from 36 degrees to 20 degrees C. 6. Preincubation with 5-HT (100 microM) caused a time-dependent and rapidly reversible decrease of the 5-HT-induced [14C]-guanidinium influx. 7. It is concluded that [14C]-guanidinium influx measurement in N1E-115 cells is a convenient method to study properties of the cation channel of the 5-HT3 receptor. This influx is independent of the fast sodium channel.
摘要
- 利用有机阳离子[14C]-胍盐，研究了5-羟色胺3（5-HT3）受体介导的阳离子流入N1E-115小鼠神经母细胞瘤细胞的过程。2. 5-羟色胺（5-HT，30微摩尔）引起[14C]-胍盐的时间依赖性流入，与藜芦碱（100微摩尔）引发的流入相反，该流入不受河豚毒素（TTX，10微摩尔）抑制。5-HT诱导的流入被P物质增强，被昂丹司琼抑制。3. 5-HT和选择性5-HT3受体激动剂间氯苯双胍、苯双胍和2-甲基-5-HT呈钟形浓度-反应曲线；效价顺序为间氯苯双胍>5-HT>苯双胍=2-甲基-5-HT。在这些激动剂中，5-HT引发的[14C]-胍盐流入最高。5-甲氧基色胺，一种5-HT4受体激动剂，无作用。4.[14C]-胍盐由100微摩尔5-HT诱导产生的流入不受麦角新碱（10微摩尔）和酮色林（10微摩尔）影响，但被5-HT3受体拮抗剂抑制，效价顺序如下：ICS 205-93 >昂丹司琼>MDL 72222 >>甲氧氯普胺。5. 在无Ca2+和/或Na+时以及温度从36℃降至20℃时，5-HT诱导的[14C]-胍盐流入增加。6. 用5-HT（100微摩尔）预孵育导致5-HT诱导的[14C]-胍盐流入呈时间依赖性且快速可逆的减少。7. 得出结论，N1E-115细胞中[14C]-胍盐流入测量是研究5-HT3受体阳离子通道特性的便捷方法。该流入与快速钠通道无关。
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