4-羟基-2-甲基-4-苯基-1,2,3,4-四氢异喹啉（PI-OH）：一种对大鼠肛门尾骨肌具有拟交感胺增强作用的新型物质。
4-Hydroxy-2-methyl-4-phenyl-1,2,3,4-tetrahydroisoquinoline (PI-OH): a new potentiator of sympathomimetic amines on the rat anococcygeus muscle.
作者信息
Ishida Y, Koga N, Nanbu T, Kihara M, Kobayashi S
机构信息
Department of Chemical Pharmacology, Faculty of Pharmaceutical Sciences, University of Tokushima, Japan.
出版信息
Br J Pharmacol. 1988 May;94(1):19-26. doi: 10.1111/j.1476-5381.1988.tb11495.x.
Abstract
- The potentiating effects of racemic 4-hydroxy-2-methyl-4-phenyl-1,2,3,4-tetrahydroisoquinoline (PI-OH), cocaine, desipramine and nomifensine on the concentration-response curves of the rat anococcygeus muscle to noradrenaline (NA) and field stimulation were examined. 2. PI-OH and cocaine concentration-dependently potentiated the responses of anococcygeus muscle to NA and field stimulation, but the activity of PI-OH was stronger than that of cocaine on both responses. 3. At high concentrations the potentiating activities of desipramine and nomifensine were less, a fact that was explained by their postsynaptic inhibitory properties; the actions of nomifensine and desipramine as antagonists against NA were competitive and non-competitive, respectively. 4. It is concluded that PI-OH may be an ideal potentiator of the response to NA in adrenergically-innervated tissues because it has no side effects such as postsynaptic inhibition.
摘要
- 研究了消旋4-羟基-2-甲基-4-苯基-1,2,3,4-四氢异喹啉（PI-OH）、可卡因、地昔帕明和诺米芬辛对大鼠肛门尾骨肌对去甲肾上腺素（NA）和场刺激的浓度-反应曲线的增强作用。2. PI-OH和可卡因浓度依赖性地增强了肛门尾骨肌对NA和场刺激的反应，但PI-OH对两种反应的活性均强于可卡因。3. 在高浓度时，地昔帕明和诺米芬辛的增强活性较小，这一事实可由它们的突触后抑制特性来解释；诺米芬辛和地昔帕明作为NA拮抗剂的作用分别是竞争性和非竞争性的。4. 得出结论，PI-OH可能是肾上腺素能神经支配组织中对NA反应的理想增强剂，因为它没有诸如突触后抑制等副作用。
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