Brown R A, Solca A M, Wilson J
J Pharm Pharmacol. 1979 Nov;31(11):761-6. doi: 10.1111/j.2042-7158.1979.tb13653.x.
The effects of differential and combined catecholamine uptake antagonism on cardiovascular responses of anaesthetized dogs to isoprenaline, noradrenaline, and electrical stimulation of the left ansa subclavia nerve have been studied. Uptake1 inhibition by cocaine HCl (5 mg kg-1 and 1 mg kg-1 every 45 min) enhanced responses to noradrenaline (0.1 to 2.0 micrograms kg-1 i.v.) and sympathetic nerve stimulation (1 to 20 Hz), but did not affect those to isoprenaline. Uptake2 inhibition by metanephrine (40 micrograms kg-1 min-1) enhanced cardiac responses to isoprenaline (0.05 to 1.0 microgram kg-1 i.v.), but did not significantly alter those to noradrenaline or nerve stimulation. Responses to all agonist interventions were increased by the combined administration of cocaine and metanephrine. Cocaine preferentially enhanced the positive chronotropic cardiac response to noradrenaline, but metanephrine did not differentiate between heart rate and contractility. These results have been discussed in the light of the mechanism of drug action involved.
研究了不同的儿茶酚胺摄取拮抗作用以及联合摄取拮抗作用对麻醉犬心血管系统对异丙肾上腺素、去甲肾上腺素以及左锁骨下袢神经电刺激反应的影响。盐酸可卡因(5mg/kg,每45分钟1mg/kg)抑制摄取1增强了对去甲肾上腺素(0.1至2.0μg/kg静脉注射)和交感神经刺激(1至20Hz)的反应,但不影响对异丙肾上腺素的反应。间甲肾上腺素(40μg/kg·min-1)抑制摄取2增强了心脏对异丙肾上腺素(0.05至1.0μg/kg静脉注射)的反应,但对去甲肾上腺素或神经刺激的反应无明显改变。可卡因和间甲肾上腺素联合给药增加了对所有激动剂干预的反应。可卡因优先增强心脏对去甲肾上腺素的正性变时反应,但间甲肾上腺素对心率和收缩力无差异作用。根据所涉及的药物作用机制对这些结果进行了讨论。