钙调蛋白拮抗剂对嗅觉环核苷酸激活电流的抑制作用。
Inhibition of olfactory cyclic nucleotide-activated current by calmodulin antagonists.
作者信息
Kleene S J
机构信息
Department of Anatomy and Cell Biology, University of Cincinnati 45267-0521.
出版信息
Br J Pharmacol. 1994 Feb;111(2):469-72. doi: 10.1111/j.1476-5381.1994.tb14760.x.
Abstract
- In amphibian olfactory receptor neurones, much of the depolarizing current in response to odours is carried by cationic channels that are directly gated by cyclic AMP. The effects of four calmodulin antagonists on the cyclic AMP-activated receptor current were studied in single olfactory cilia of the frog. 2. Two antagonists, W-7 and trifluoperazine, were potent and reversible inhibitors of the cyclic AMP-activated current. IC50 values were 5 microM for W-7 and 13 microM for trifluoperazine. A third antagonist, calmidazolium, irreversibly blocked the current. The fourth, mastoparan, had little effect. 3. Calmodulin was unable to reverse the effects of W-7 and trifluoperazine, suggesting that these inhibitors act directly on the cyclic AMP-gated channels. 4. Neither W-7 nor trifluoperazine inhibited a Ca(2+)-activated Cl- current which also contributes to the odorant response. These compounds thus allow the two components of the olfactory receptor current to be discriminated.
摘要
- 在两栖动物嗅觉受体神经元中，对气味产生反应的大部分去极化电流由直接受环磷酸腺苷（cAMP）门控的阳离子通道传导。在青蛙的单个嗅觉纤毛中研究了四种钙调蛋白拮抗剂对cAMP激活的受体电流的影响。2. 两种拮抗剂，W-7和三氟拉嗪，是cAMP激活电流的强效可逆抑制剂。W-7的半数抑制浓度（IC50）值为5微摩尔，三氟拉嗪为13微摩尔。第三种拮抗剂，氯米帕明，不可逆地阻断电流。第四种，马斯托帕兰，几乎没有作用。3. 钙调蛋白无法逆转W-7和三氟拉嗪的作用，表明这些抑制剂直接作用于cAMP门控通道。4. W-7和三氟拉嗪均未抑制同样对气味反应有贡献的钙激活氯电流。因此，这些化合物可以区分嗅觉受体电流的两个组成部分。
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