Krasnikova T L, Iurkova V B, Ku'zmina M M, Ku'lginskaia I V, Sokolov S F, Golitsyn S I, Chernousova T V, Svet E A, Mazaev A V
Kardiologiia. 1989 Jul;29(7):25-9.
The authors analyzed the density of beta 2-adrenoreceptors, their affinity for catecholamines and activity of peripheral lymphocyte adenylate cyclase in healthy donors and patients with frequent ventricular premature contraction (VPC) in their pretreatment state and during short-term ethmosine or allapinine therapy. The density of beta 2-adrenoreceptors was increased by 43%, whereas guanylimidodiphosphate- or forskolin-induced stimulation of adenylate cyclase was decreased in the lymphocytes of VPC patients as compared to those of healthy donors. Ethmosine therapy failed to produce any changes in the density and affinity of the receptors for catecholamines. Allapinine caused a 47% reduction in beta 2-adrenoreceptor density and a 10(2)-10(3)-fold decrease in receptor affinity for 1-isoproterenol. After discontinuation of allapinine, the changes in beta 2-adrenoreceptor density and affinity for catecholamines remained on days 3 and 7, respectively. The clinical effect of both ethmosine and allapinine was accompanied by an increase in lymphocyte adenylate cyclase activity.
作者分析了健康供体以及频发室性早搏（VPC）患者在治疗前状态和短期使用乙胺碘呋酮或阿拉丙宁治疗期间β2 - 肾上腺素能受体的密度、它们对儿茶酚胺的亲和力以及外周淋巴细胞腺苷酸环化酶的活性。与健康供体相比，VPC患者淋巴细胞中β2 - 肾上腺素能受体的密度增加了43%，而鸟苷亚氨基二磷酸或福斯可林诱导的腺苷酸环化酶刺激作用减弱。乙胺碘呋酮治疗未能使儿茶酚胺受体的密度和亲和力发生任何变化。阿拉丙宁使β2 - 肾上腺素能受体密度降低了47%，并且受体对1 - 异丙肾上腺素的亲和力降低了10² - 10³倍。停用阿拉丙宁后，β2 - 肾上腺素能受体密度和对儿茶酚胺亲和力的变化分别在第3天和第7天仍持续存在。乙胺碘呋酮和阿拉丙宁的临床疗效均伴随着淋巴细胞腺苷酸环化酶活性的增加。
