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首页> 外文期刊>Canadian Journal of Physiology and Pharmacology >Specific binding of (3H)ketanserin to hypothalamus membranes of juvenile rainbow trout, Oncorhynchus mykiss.
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Specific binding of (3H)ketanserin to hypothalamus membranes of juvenile rainbow trout, Oncorhynchus mykiss.

机译：（3H）酮色林与幼年虹鳟Oncorhynchus mykiss的下丘脑膜的特异性结合。

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摘要

This study examines the existence and pharmacological specificity of [3H]ketanserin binding in hypothalamus of juvenile rainbow trout. Hypothalamic membranes were incubated with [3H]ketanserin (selective 5HT2 antagonist) under several experimental conditions; reactions were terminated by filtration and bound radioactivity was counted by liquid scintillation spectroscopy. Tissue dilution experiments revealed that specific [3H]ketanserin binding (B(sp)) was tissue dependent; 1 hypothalamus equivalent per tube (1100 +/- 115 cpm/mg protein) was subsequently used throughout the rest of this study. In association experiments, B(sp) increased progressively with time, achieved equilibrium binding levels (1192 +/- 120 cpm/mg protein) within 80 min, and remained stable for at least 60 min thereafter; k(obs), and k(+1) were 0.032 and 0.048 min(-1) x nM(-1), respectively. In dissociation experiments, B(sp) completely dissociated within 20 min following addition of excess ketanserin; k(-1) and t1/2 were 0.0803 min(-1) and 8.7 min, respectively. B(sp) was saturable (2500 +/- 256 cpm/mg protein); Scatchard-calculated values for the equilibrium dissociation constant (K(D)) and capacity (Bmax) were 0.48 nM, and 125 fmol/mg protein, respectively. B(sp) was differentially displaced by structurally related competitors, with a rank order of potency of ketanserin = mianserin > ritanserin > serotonin (5HT) = spiperone methiothepin mesylate > metergoline = DOI ((+/-)-2-5-dimethoxy-4-iodoamphetamine hyrobromide) > 2-methyl-5HT > alpha-methyl-5HT 5HIAA (5-hydroxyindole acetic acid) = reserpine. These findings provide pharmacological evidence for the presence of a 5HT2-like receptor subtype in the trout hypothalamus.
机译：这项研究审查了[3H]酮色林结合在少年虹鳟的下丘脑中的存在及其药理学特异性。下丘脑膜与[3H] ketanserin（选择性5HT2拮抗剂）在几种实验条件下孵育;通过过滤终止反应，并通过液体闪烁光谱法计数结合的放射性。组织稀释实验表明，特定的[3H]酮色林结合（B（sp））是组织依赖性的;在本研究的其余部分中，随后每管使用1个下丘脑当量（1100 +/- 115 cpm / mg蛋白）。在关联实验中，B（sp）随时间逐渐增加，在80分钟内达到平衡结合水平（1192 +/- 120 cpm / mg蛋白质），此后至少稳定60分钟; k（obs）和k（+1）分别为0.032和0.048 min（-1）x nM（-1）。在解离实验中，添加过量的酮色林后20分钟内B（sp）完全解离; k（-1）和t1 / 2分别为0.0803分钟（-1）和8.7分钟。 B（sp）是饱和的（2500 +/- 256 cpm / mg蛋白质）; Scatchard计算的平衡解离常数（K（D））和容量（Bmax）分别为0.48 nM和125 fmol / mg蛋白质。 B（sp）被结构上相关的竞争者以不同的方式置换，酮色林=米安色林>利坦色林>血清素（5HT）=哌隆甲硫基甲磺酸甲磺酸盐>美特古琳= DOI（（+/-）-2-5-二甲氧基-4-碘苯丙胺氢溴酸盐）> 2-甲基-5HT>α-甲基-5HT 5HIAA（5-羟基吲哚乙酸）=利血平。这些发现为鳟鱼下丘脑中存在5HT2样受体亚型提供了药理学证据。

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