Fozard J R, Berry J L
Pharmacology. 1976;14(4):357-61. doi: 10.1159/000136615.
Rabbit hearts removed 3H-5-hydroxytryptamine (3H-5-HT) from a perfusion concentration of 2.6 X 10(-9) g/ml. 15.8% of the extractable cardiac total radioactivity consisted of metabolites, mainly 5-hydroxyindoleacetic acid, and metabolism appeared in the perfusion fluid during the course of the perfusion. Ergotamine tartrate (1.0 X 10(-6) g/ml) caused a small increase in 3H-5-HT uptake by the heart. Methysergide bimaleate (1.0 X 10(-6) g/ml) slowed the appearance of metabolites in the perfusion fluid. Because of the high concentrations required, neither observation seems likely to be of clinical significance to migraine. The results do, however, suggest that the frequently observed sensitisation of tissues to 5-HT by ergotamine and methysergide is not the result of inhibition of its tissue uptake.
兔心脏从灌注浓度为2.6×10⁻⁹克/毫升的溶液中清除3H - 5 - 羟色胺(3H - 5 - HT)。可提取的心脏总放射性的15.8%由代谢物组成,主要是5 - 羟吲哚乙酸,并且在灌注过程中代谢物出现在灌注液中。酒石酸麦角胺(1.0×10⁻⁶克/毫升)使心脏对3H - 5 - HT的摄取略有增加。马来酸甲麦角新碱(1.0×10⁻⁶克/毫升)减缓了代谢物在灌注液中的出现。由于需要高浓度,这两种观察结果似乎对偏头痛都不太可能具有临床意义。然而,这些结果确实表明,麦角胺和甲麦角新碱经常观察到的组织对5 - HT的致敏作用不是抑制其组织摄取的结果。