Guimarães S, Azevedo I, Cardoso W, Oliveira M C
Naunyn Schmiedebergs Arch Pharmacol. 1975;286(4):401-12. doi: 10.1007/BF00506654.
The relation between the smooth muscle cell mass of dog saphenous vein strips and the degree of supersensitivity to isoprenaline caused by U-0521 (3,4-dihydroxy-2-methyl propiophenone), an inhibitor of the catechol-O-methyl transferase (COMT), was studied. For the quantitative determination of smooth muscle mass, the thickness of the muscle layer as determined by light microscopy and the maximal shortening induced by supramaximal concentration of phenylephrine were used. After the strips had been contracted by 3x10-6M phenylephrine, a concentration which was able to produce an about 90% maximal contraction, dose-response curves to the relaxant effect of isoprenaline were determined in the absence and in the presence of U-0521 (10-4M). It was observed that U-0521 caused marked supersensitivity to the relaxant effect of isoprenaline (varying between 3 and 81 times), as well as an increase of the maximal relaxation caused by this amine (varying between 7 and 120%). The correlation between these data and the smooth muscle cell mass shows that there was a direct proportionality between these parameters. Oxytetracycline (10-4M), an inhibitor of binding of catecholamines to collagen, did not produce any enhancement of the effects of isoprenaline. It is concluded that COMT is related to smooth muscle cells in this tissue.
研究了犬隐静脉条平滑肌细胞质量与儿茶酚 - O - 甲基转移酶(COMT)抑制剂U - 0521(3,4 - 二羟基 - 2 - 甲基苯丙酮)引起的对异丙肾上腺素超敏反应程度之间的关系。为了定量测定平滑肌质量,使用了通过光学显微镜测定的肌层厚度以及去氧肾上腺素超最大浓度诱导的最大缩短量。在用3×10⁻⁶M去氧肾上腺素使条带收缩后(该浓度能够产生约90%的最大收缩),在不存在和存在U - 0521(10⁻⁴M)的情况下,测定了对异丙肾上腺素舒张作用的剂量 - 反应曲线。观察到U - 0521导致对异丙肾上腺素舒张作用的明显超敏反应(变化范围在3至81倍之间),以及该胺引起的最大舒张增加(变化范围在7至120%之间)。这些数据与平滑肌细胞质量之间的相关性表明,这些参数之间存在直接比例关系。土霉素(10⁻⁴M),一种儿茶酚胺与胶原蛋白结合的抑制剂,未产生异丙肾上腺素作用的任何增强。得出的结论是,COMT与该组织中的平滑肌细胞有关。