Altar C A, Wasley A M, Martin L L
Neuroscience. 1986;17(1):263-73. doi: 10.1016/0306-4522(86)90241-1.
The distribution and pharmacological specificity of [3H]tryptamine binding to coronal and horizontal sections of the rat brain were investigated with computer-assisted autoradiography. [3H]Tryptamine bound to brain regions with up to 58% specificity, as determined with 10 microM tryptamine as a displacer. The capacity (Bmax) of saturable [3H]tryptamine binding sites was greatest in the nucleus accumbens and claustrum (660-760 fmol mg protein-1), with intermediate binding site concentrations in hippocampus, septum, olfactory tubercle, frontal cortex, cingulate cortex and caudate-putamen. The phenylalkylamine, p-methoxyphenylpropylamine and the beta-carboline, harmaline, as well as 5-methyl-tryptamine, displaced [3H]tryptamine from each of these brain regions with a potency that approximated the 5-9 nM affinity (Kd) of [3H]tryptamine binding to each site. Only micromolar concentrations of serotonin displaced [3H]tryptamine, which did not bind to S1, S2, D1, D2 or alpha- or beta-adrenergic sites. The unique pharmacology and the regional overlap of [3H]tryptamine binding sites with dopaminergic nerve terminals in the nucleus accumbens and caudate-putamen suggest that tryptamine-containing neurons in the mammalian brain may modulate behavioral functions such as locomotion.
采用计算机辅助放射自显影技术，研究了[3H]色胺与大鼠脑冠状和水平切片结合的分布及药理学特异性。以10微摩尔色胺作为置换剂测定，[3H]色胺与脑区结合的特异性高达58%。可饱和的[3H]色胺结合位点的容量（Bmax）在伏隔核和屏状核中最大（660 - 760飞摩尔/毫克蛋白-1），海马、隔区、嗅结节、额叶皮质、扣带回皮质和尾状核-壳核中的结合位点浓度处于中等水平。苯烷基胺、对甲氧基苯丙胺、β-咔啉、哈尔满以及5-甲基色胺，能以接近[3H]色胺与各位点5 - 9纳摩尔亲和力（Kd）的效力，从这些脑区置换[3H]色胺。只有微摩尔浓度的5-羟色胺能置换[3H]色胺，且[3H]色胺不与S1、S2、D1、D2或α-或β-肾上腺素能位点结合。[3H]色胺结合位点在伏隔核和尾状核-壳核中独特的药理学特性以及与多巴胺能神经末梢的区域重叠表明，哺乳动物脑中含色胺的神经元可能调节诸如运动等行为功能。
