Packham Rachel, Walker Robert J, Holden-Dye Lindy
School of Biological Sciences, University of Southampton, Highfield Campus, Life Sciences Building 85, Southampton, SO17 1BJ, UK.
Invert Neurosci. 2010 Nov;10(1):47-52. doi: 10.1007/s10158-010-0107-9. Epub 2010 Oct 22.
This paper investigates the effect of epinastine, a selective octopamine antagonist in invertebrates, in Caenorhabditis elegans. Specifically, its ability to block the inhibitory action of octopamine on C. elegans-isolated pharynx was assayed. Isolated pharynxes were stimulated to pump by the addition of 500 nM 5-hydroxytryptamine (5-HT) (113 ± 2 per 30 s, n = 15). Octopamine inhibited the 5-HT-induced pumping in a concentration-dependent manner (threshold 1-5 μM) with a 61 ± 11% inhibition with 50 μM (n = 5). Epinastine (0.1 μM) antagonized the inhibitory response to octopamine (P < 0.001; n = 15). Tyramine also inhibited pharyngeal pumping induced by 5-HT but was less potent than octopamine. Tyramine, 50 μM to 1 mM, gave a transient inhibition e.g. of 40 ± 5% at 50 μM (n = 5). A higher (10 μM) concentration of epinastine was required to block the tryamine response compared with octopamine. It is concluded that epinastine selectively antagonizes the effect of octopamine on C. elegans pharynx. Further studies are required to test its selectivity for octopamine in other tissues and other nematodes.
本文研究了一种无脊椎动物中的选择性章鱼胺拮抗剂依匹斯汀对秀丽隐杆线虫的作用。具体而言,检测了其阻断章鱼胺对秀丽隐杆线虫分离咽部抑制作用的能力。通过添加500 nM 5-羟色胺(5-HT)刺激分离的咽部进行泵吸(每30秒113±2次,n = 15)。章鱼胺以浓度依赖性方式抑制5-HT诱导的泵吸(阈值1-5μM),50μM时抑制率为61±11%(n = 5)。依匹斯汀(0.1μM)拮抗对章鱼胺的抑制反应(P < 0.001;n = 15)。酪胺也抑制5-HT诱导的咽部泵吸,但效力低于章鱼胺。50μM至1 mM的酪胺产生短暂抑制,例如50μM时为40±5%(n = 5)。与章鱼胺相比,需要更高浓度(10μM)的依匹斯汀来阻断酪胺反应。得出的结论是,依匹斯汀选择性拮抗章鱼胺对秀丽隐杆线虫咽部的作用。需要进一步研究以测试其在其他组织和其他线虫中对章鱼胺的选择性。