Bevan P, Bradshaw C M, Pun R Y, Slater N T, Szabadi E
Br J Pharmacol. 1978 Aug;63(4):651-7. doi: 10.1111/j.1476-5381.1978.tb17278.x.
1 The technique of microelectrophoresis was used in order to compare the actions of tyramine and noradrenaline on single neurones in the cerebral cortex of the rat.2 Tyramine could both excite and depress cortical neurones. Each tyramine-sensitive cell was also sensitive to noradrenaline. There was a high correlation between the directions of responses to tyramine and noradrenaline, most cells excited by tyramine being excited by noradrenaline, and most cells depressed by tyramine being depressed by noradrenaline.3 In the case of both excitatory and depressant responses, tyramine appeared to be less potent than noradrenaline.4 Tyramine evoked ;slower' responses than noradrenaline, both the latencies to onset and the recovery times being longer for responses to tyramine than for responses to noradrenaline.5 When the rates of release of tyramine and noradrenaline from micropipettes were measured in vitro, no significant difference could be observed between the transport numbers of the two drugs. Thus the difference in potency between the two drugs, and the difference in the time courses of responses to the two drugs, are presumably of biological origin.6 Desipramine could discriminate between neuronal responses to tyramine and noradrenaline: responses to tyramine were antagonized, while responses to noradrenaline were either potentiated or unaffected. Responses to DL-homocysteic acid were not affected by desipramine.7 The results are consistent with the hypothesis that tyramine is an indirectly acting sympathomimetic amine in the brain, and desipramine acts by blocking the uptake of both tyramine and noradrenaline into presynaptic noradrenergic nerve terminals.
采用微电泳技术比较酪胺和去甲肾上腺素对大鼠大脑皮层单个神经元的作用。
酪胺可兴奋和抑制皮层神经元。每个对酪胺敏感的细胞也对去甲肾上腺素敏感。对酪胺和去甲肾上腺素的反应方向之间存在高度相关性,大多数被酪胺兴奋的细胞也被去甲肾上腺素兴奋,大多数被酪胺抑制的细胞也被去甲肾上腺素抑制。
在兴奋和抑制反应的情况下,酪胺的作用似乎比去甲肾上腺素弱。
酪胺引起的反应比去甲肾上腺素“慢”,酪胺反应的起始潜伏期和恢复时间都比去甲肾上腺素反应的长。
当在体外测量从微量移液器释放酪胺和去甲肾上腺素的速率时,两种药物的转运数之间未观察到显著差异。因此,两种药物效力的差异以及对两种药物反应的时间进程差异可能源于生物学因素。
地昔帕明可区分神经元对酪胺和去甲肾上腺素的反应:对酪胺的反应被拮抗,而对去甲肾上腺素的反应要么增强要么不受影响。对DL-高胱氨酸的反应不受地昔帕明影响。
这些结果与以下假设一致:酪胺是脑中一种间接作用的拟交感胺,地昔帕明通过阻断酪胺和去甲肾上腺素进入突触前去甲肾上腺素能神经末梢的摄取而起作用。