Imipramine inhibits Cl(-) secretion by desensitization of beta-adrenergic receptors in calu-3 human airway cells.
Imipramine inhibits Cl(-) secretion by desensitization of beta-adrenergic receptors in calu-3 human airway cells.
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Imipramine 通过使 calu-3 人气道细胞中的 β-肾上腺素能受体脱敏来抑制 Cl(-) 分泌。
DOI：
10.1006/bbrc.2000.3202
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发表时间：
2000
影响因子：
3.1
通讯作者：
K. Yamaki
中科院分区：
文献类型：
--
作者：
Y. Mizuno;Y. Ito;M. Aoyama;H. Kume;S. Nakayama;K. Yamaki
最近的研究发现，像丙咪嗪（IMP）这样的四环抗抑郁药不仅在大脑中有高亲和力位点，而且在哺乳动物的肺中也有高亲和力位点。在本研究中，我们检测了IMP对Calu-3人气道细胞中β -肾上腺素能受体（β - ar）激动剂异丙肾上腺素（ISP）分泌Cl（-）的影响。在基底侧溶液中应用ISP会产生持续的短路电流，该电流被二苯胺-2-羧酸盐（一种Cl（-）通道阻滞剂）消除。IMP （0.01-1 mM）在根尖或基底侧溶液中作用30 min，均呈浓度依赖性地显著抑制isp诱导的反应，且从根尖而非基底侧作用时，抑制作用更为显著。这些结果表明，在Calu-3细胞中，IMP能从胞质侧使基底侧膜上的β - ar脱敏。
Recent investigations have found that tetracyclic antidepressants like imipramine (IMP) have high-affinity sites not only in brain but also in mammalian lung. In the present study, we examined the effects of IMP on the Cl(-) secretion produced by isoproterenol (ISP), a beta-adrenergic receptor (beta-AR) agonist, in Calu-3 human airway cells. ISP applied in the basolateral solution generated a sustained short-circuit current that was abolished by diphenylamine-2-carboxylate, a Cl(-) channel blocker. IMP (0.01-1 mM) applied in the apical or basolateral solution for 30 min significantly inhibited the ISP-induced responses in a concentration-dependent manner, and the inhibitory effects of this drug were remarkable when applied from the apical rather than the basolateral side. ISP-induced responses were mimicked by forskolin- and 8-bromo-cyclic AMP-induced ones, but which were insensitive to IMP. These results indicate that IMP desensitizes the beta-AR on the basolateral membrane from the cytosolic side in Calu-3 cells.
大鼠脑中丙咪嗪诱导的β肾上腺素能受体下调的时间过程的神经解剖学特异性和剂量依赖性。
DOI：
--
发表时间：
1994
期刊：
The Journal of pharmacology and experimental therapeutics
影响因子：
--
作者：
Duncan,GE;Knapp,DJ;Little,KY;Breese,GR
通讯作者：
Breese,GR
丙咪嗪对小鼠背根神经节神经元中 L 型钙通道的选择性抑制涉及 G 蛋白。
DOI：
--
发表时间：
1992
期刊：
The Journal of pharmacology and experimental therapeutics
影响因子：
--
作者：
Choi,JJ;Huang,GJ;Shafik,E;Wu,WH;McArdle,JJ
通讯作者：
McArdle,JJ