van Hooft J A, Kreikamp A P, Vijverberg H P
Research Institute of Toxicology, Utrecht University, The Netherlands.
J Neurochem. 1997 Sep;69(3):1318-21. doi: 10.1046/j.1471-4159.1997.69031318.x.
Efficacies of the 5-hydroxytryptamine (serotonin) 5-HT3 receptor (5-HT3R) agonists 2-methyl-5-HT, dopamine, and m-chlorophenylbiguanide on 5-HT3R native to N1E-115 cells and on homopentameric 5-HT3R expressed in Xenopus oocytes were determined relative to that of 5-HT. Efficacies of 2-methyl-5-HT and dopamine on 5-HT3R native to differentiated N1E-115 cells are high (54 and 36%) as compared with their efficacies on homopentameric 5-HT3R-A(L) and 5-HT3R-A(S) receptors expressed in oocytes (4-8%). m-Chlorophenylbiguanide does not distinguish between 5-HT3R in N1E-115 cells and in oocytes. The distinct pharmacological profile of 5-HT3R native to differentiated N1E-115 cells is conserved when poly(A)+ mRNA from these cells is expressed in oocytes. The results indicate that, apart from the known 5-HT3R subunits, N1E-115 cells express additional proteins involved in 5-HT3R function.
相对于5-羟色胺(血清素),测定了5-羟色胺(5-HT)3受体(5-HT3R)激动剂2-甲基-5-HT、多巴胺和间氯苯双胍对N1E-115细胞天然存在的5-HT3R以及非洲爪蟾卵母细胞中表达的同五聚体5-HT3R的作用效果。与它们对卵母细胞中表达的同五聚体5-HT3R-A(L)和5-HT3R-A(S)受体的作用效果(4%-8%)相比,2-甲基-5-HT和多巴胺对分化的N1E-115细胞天然存在的5-HT3R的作用效果较高(分别为54%和36%)。间氯苯双胍无法区分N1E-115细胞和卵母细胞中的5-HT3R。当这些细胞的聚腺苷酸加尾(poly(A)+)mRNA在卵母细胞中表达时,分化的N1E-115细胞天然存在的5-HT3R独特的药理学特征得以保留。结果表明,除了已知的5-HT3R亚基外,N1E-115细胞还表达参与5-HT3R功能的其他蛋白质。