一种对可卡因敏感的果蝇血清素转运体：克隆、表达及电生理学特性分析
A cocaine-sensitive Drosophila serotonin transporter: cloning, expression, and electrophysiological characterization.
作者信息
Corey J L, Quick M W, Davidson N, Lester H A, Guastella J
机构信息
Division of Biology 156-29, California Institute of Technology, Pasadena 91125.
出版信息
Proc Natl Acad Sci U S A. 1994 Feb 1;91(3):1188-92. doi: 10.1073/pnas.91.3.1188.
Abstract
A cocaine-sensitive, high-affinity Drosophila serotonin (5-hydroxytryptamine; 5HT) transporter cDNA, denoted dSERT1, was isolated and characterized in oocytes. dSERT1 shows little transport of other monoamines and is Na+ and Cl- dependent. Sequence analysis indicates 12 putative transmembrane domains and strong homologies (approximately 50%) among dSERT1 and mammalian 5HT, norepinephrine, and dopamine transporters. Interestingly, the pharmacological properties of dSERT1, including sensitivity to antidepressants, are more similar to those of mammalian catecholamine transporters than to mammalian 5HT transporters. Two-electrode voltage-clamp analysis demonstrated 5HT-induced, voltage-dependent currents. Cloning and characterization of dSERT1 adds significantly to our knowledge of the diversity of 5HT transporters with regard to primary sequence, pharmacological profile, and permeation properties.
摘要
在卵母细胞中分离并鉴定了一种对可卡因敏感、具有高亲和力的果蝇血清素（5-羟色胺；5HT）转运体cDNA，命名为dSERT1。dSERT1对其他单胺类物质的转运作用很小，且依赖于Na+和Cl-。序列分析表明，dSERT1具有12个假定的跨膜结构域，与哺乳动物的5HT、去甲肾上腺素和多巴胺转运体具有很强的同源性（约50%）。有趣的是，dSERT1的药理学特性，包括对抗抑郁药的敏感性，与哺乳动物儿茶酚胺转运体的特性比与哺乳动物5HT转运体的特性更相似。双电极电压钳分析显示了5HT诱导的电压依赖性电流。dSERT1的克隆和鉴定显著增加了我们对5HT转运体在一级序列、药理学特征和通透特性方面多样性的认识。
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