Oliveira L F, Bretas A D, Sudo R T
Gen Pharmacol. 1976 Aug;7(2-3):189-93. doi: 10.1016/0306-3623(76)90060-4.
The effects of 5-hydroxytriptamine (5-HT), 5-HT blocking agents, morphine, narcotic-antagonists and ganglionic blocking agents were tested in the dog intestine by close intra-arterial injection. Morphine, as 5-HT, induced an immediate increase in the intestinal tonus followed by phasic contractions. When 5-HT was injected immediately after cessation of morphine induced phasic contractions, a significant potentiation of the 5-HT induced intestinal contraction could be observed. The potentiation could be demonstrated for other narcotic-analgesics like dextromoramide and it is specific for 5-HT. 5-HT blocking agents like LSD, BOL, and cyproheptadine did not block either 5-HT or morphine. However, bufotenidine, a neural tryptaminergic blocking agent, blocked the effects of both 5-HT and morphine. The effects of 5-HT and morphine upon intestinal motility were also diminished by ganglionic depolarizing agents such as nicotine and DMPP. This effect could, however, be prevented by the pretreatment with hexamethonium. These results seem to confirm the hypothesis of a 5-HT mediator role in the intestinal contractile effect induced by the narcotic-analgesics. On the other hand, narcotic-antagonists such as nalorphine and cyclazocine, not only lacked the 5-HT potentiation effect but also prevented the 5-HT potentiation induced by morphine. Cyclazocine also showed a long lasting 5-HT blocking effect. These results seem to show that the 5-HT potentiating effect of morphine in vivo is very specific and characteristic of the narcotics and thus could be implicated in some of their central effects.
通过动脉内近距离注射,在犬肠中测试了5-羟色胺(5-HT)、5-HT阻断剂、吗啡、麻醉拮抗剂和神经节阻断剂的作用。吗啡与5-HT一样,可立即引起肠张力增加,随后出现阶段性收缩。当在吗啡诱导的阶段性收缩停止后立即注射5-HT时,可观察到5-HT诱导的肠收缩有明显增强。这种增强作用在其他麻醉性镇痛药如右吗拉胺中也可得到证实,且对5-HT具有特异性。5-HT阻断剂如麦角酸二乙酰胺(LSD)、丁酰苯类(BOL)和赛庚啶既不阻断5-HT也不阻断吗啡。然而,神经色胺能阻断剂蟾蜍特宁可阻断5-HT和吗啡的作用。烟碱和二甲基苯基哌嗪(DMPP)等神经节去极化剂也可减弱5-HT和吗啡对肠运动的作用。不过,六甲铵预处理可预防这种作用。这些结果似乎证实了5-HT作为介质在麻醉性镇痛药诱导的肠收缩效应中起作用的假说。另一方面,纳洛芬和环唑辛等麻醉拮抗剂不仅缺乏5-HT增强作用,而且还可阻止吗啡诱导的5-HT增强作用。环唑辛还表现出持久的5-HT阻断作用。这些结果似乎表明,吗啡在体内的5-HT增强作用非常特异,是麻醉药的特征,因此可能与它们的一些中枢作用有关。