Joiner P D, Kadowitz P J, Davis L B, Hyman A L
Can J Physiol Pharmacol. 1975 Oct;53(5):830-8. doi: 10.1139/y75-114.
Isolated helical strips of canine intrapulmonary lobar arteries and veins (about 4 mm in diameter) undergo dose-related tension development when exposed to increasing concentrations (10(-8) - 10(-3) M) of norepinephrine (NE), serotonin or 5-hydroxytryptamine (5-HT) and tyramine (Tyr). Venous segments were generally more sensitive while the maximum tension development was greater in the arterial strips, probably owing to their greater thickness. Both strips were more sensitive to 5-HT than NE and only responded to Tyr at high concentrations. Norepinephrine and 5-HT were nearly equally efficacious, whereas Tyr was less so. Responses to the latter were slow to develop, exhibited tachyphylaxis, and were greatly inhibited by phentolamine (10(-8) M), an alpha-adrenergic blocker. Exposure to cocaine (10(-5) M) enhanced submaximal NE responses, inhibited Tyr contractions and had no consistent effect on 5-HT responses. Phentolamine (10(-8) M) was also found to inhibit NE responses without altering 5-HT probably acts on other receptors. Tyramine may, in part, act directly on alpha-adrenergic receptors but may also release NE from surviving adrenergic nerve terminals in the preparation. Cocaine inhibits this effect and potentiates responses to lower levels of NE, presumably by blocking NE uptake into nerve terminals although a post-junctional action cannot be excluded.
将犬肺内叶动脉和静脉的孤立螺旋条带(直径约4毫米)暴露于去甲肾上腺素(NE)、血清素或5-羟色胺(5-HT)以及酪胺(Tyr)浓度不断增加(10⁻⁸ - 10⁻³ M)的环境中时,它们会出现与剂量相关的张力变化。静脉段通常更敏感,而动脉条带中的最大张力变化更大,这可能是由于其厚度更大。两种条带对5-HT的敏感性均高于NE,且仅在高浓度时对Tyr有反应。去甲肾上腺素和5-HT的效力几乎相同,而酪胺的效力则较弱。对后者的反应发展缓慢,表现出快速耐受性,并且被α-肾上腺素能阻滞剂酚妥拉明(10⁻⁸ M)大大抑制。暴露于可卡因(10⁻⁵ M)可增强次最大NE反应,抑制Tyr收缩,并且对5-HT反应没有一致的影响。还发现酚妥拉明(10⁻⁸ M)可抑制NE反应而不改变5-HT,这可能作用于其他受体。酪胺可能部分直接作用于α-肾上腺素能受体,但也可能从制剂中存活的肾上腺素能神经末梢释放NE。可卡因抑制这种作用并增强对较低水平NE的反应,推测是通过阻断NE摄取到神经末梢,尽管不能排除其对节后的作用。