SEROTONIN BINDING PROTEIN: ENHANCEMENT OF BINDING BY Fe2+ AND INHIBITION OF BINDING BY DRUGS 1 2
SEROTONIN BINDING PROTEIN: ENHANCEMENT OF BINDING BY Fe2+ AND INHIBITION OF BINDING BY DRUGS 1 2
复制标题
血清素结合蛋白：Fe2 结合的增强和药物结合的抑制 1 2
DOI：
10.1111/j.1471-4159.1976.tb06467.x
复制
发表时间：
1976
影响因子：
4.7
通讯作者：
M. Rapport
中科院分区：
文献类型：
--
作者：
H. Tamir;A. Klein;M. Rapport
5-羟色胺与存在于突触体中并与多巴胺能束相关的可溶性高亲和力结合蛋白的结合，现在已经研究了金属离子和各种药物的作用。在Fe 2+的最佳浓度（10 - 4 M）下，结合增强接近20倍。Cu 2+的影响要小得多。对于其它离子（Fe 3+、Mn 2+、Co2+、Ni 2+、Cr 3+、Mg 2+、Ca 2+），观察到很少或没有影响。Fe ~（2+）的影响。需要预孵育（10 min，25°C），浓度高于10 - 4 M时具有抑制作用。基于平衡透析的研究表明，Fe 2+的影响是对5-羟色胺与蛋白质结合的亲和力，而不是对结合能力的影响。在pH 8.6的聚丙烯酰胺凝胶中，在存在Fe 2+的情况下形成的血清素-蛋白质复合物的迁移性质不同于在不存在Fe 2+的情况下形成的复合物的迁移性质。核苷酸（ATP、GTP、ADP、AMP）抑制THC结合。还研究了几类药物（生物胺储存和摄取抑制剂、拟精神病药、MAO抑制剂和与收缩蛋白结合的药物）的作用。5-羟色胺结合的唯一有效抑制剂是利血平、长春碱和CZ-74，其分别在2 × 10 - 6 M、7.5 × 10 - 6 M和0.2 × 10 - 6 M下引起50%抑制。
The binding of serotonin to a soluble, high affinity binding protein, present in synaptosomes and associated with serotonergic tracts, has now been studied for the effects of metallic ions and various drugs. At optimal concentration (10‐4 M) of Fe2+ the enhancement of binding was close to 20‐fold. A much smaller effect was noted with Cu2+. With other ions (Fe3+, Mn2+, Co2+, Ni2+, Cr3+, Mg2+, Ca2+) little or no effect was seen. For the effect with Fe2+. preincubation was required (10 min, 25°C) and concentrations higher than 10‐4M were inhibitory. Studies based on equilibrium dialysis show that the effect of Fe2+ was on the affinity of the binding of serotonin to the protein, rather than on the binding capacity. In polydcrylamide gels at pH 8.6 the migratory properties of thc serotonin‐protein complex formed in the presence of Fe2+ differ from those of the complex formed without Fe2+. Nucleotides (ATP, GTP, ADP, AMP) inhibited thc binding. The effects of several classes of drugs (inhibitors of biogenic amine storage and uptake, psychotomimetics, MAO) inhibitors and drugs binding to contractile proteins) were also studied. The only effective inhibitors of serotonin binding were reserpine, vinblastine and CZ‐74, which caused 50% inhibition at 2 × 10‐6 M, 7.5 × 10‐6 M and 0.2 × 10‐6M respectively.