麻醉性镇痛药对血小板摄取5-羟色胺和（-）-间羟胺的影响。
The effect of narcotic analgesics on the uptake of 5-hydroxytryptamine and (-)-metaraminol by blood platelets.
作者信息
Ahtee L, Saarnivaara L
出版信息
Br J Pharmacol. 1973 Apr;47(4):808-18. doi: 10.1111/j.1476-5381.1973.tb08208.x.
Abstract
- The effects of narcotic analgesic and related drugs were studied on the uptake of 5-hydroxytryptamine (5-HT) and (-)-metaraminol by blood platelets.2. The most potent drug in inhibiting the uptake of 5-HT (10 muM) by human platelets was methadone, followed by pentazocine>piminodine approximately pethidine approximately anileridine approximately cyclazocine approximately thebaine > dextropropoxyphene. Alphaprodine, papaverine, apomorphine, nalorphine, codeine, and morphine were almost without effect. Methadone was slightly less active than desipramine, and had 10% of the activity of imipramine under similar conditions. Naloxone did not antagonize the effect of methadone on 5-HT uptake.3. The most potent inhibitor of metaraminol (3 muM) uptake by human platelets was piminodine, followed by pentazocine>/=anileridine>cyclazocine=methadone > dextropropoxyphene approximately thebaine >/= papaverine approximately alphaprodine >pethidine>morphine. The activity of morphine was 1% of that of piminodine. Piminodine was more potent than desipramine and protriptyline under similar conditions. The order of potency of drugs studied in inhibiting the uptake of metaraminol by rabbit platelets was similar to that obtained with human platelets.4. The effects of the analgesics studied on inhibiting uptake of monoamines did not correlate with their pain-relieving properties.
摘要
研究了麻醉性镇痛药及相关药物对血小板摄取5-羟色胺（5-HT）和（-）-间羟胺的影响。
抑制人血小板摄取5-HT（10μM）最有效的药物是美沙酮，其次是喷他佐辛＞匹米诺定≈哌替啶≈阿尼利定≈环唑辛≈蒂巴因＞右丙氧芬。阿法罗定、罂粟碱、阿扑吗啡、烯丙吗啡、可待因和吗啡几乎没有作用。美沙酮的活性略低于地昔帕明，在相似条件下其活性为丙咪嗪的10%。纳洛酮不能拮抗美沙酮对5-HT摄取的作用。
抑制人血小板摄取间羟胺（3μM）最有效的抑制剂是匹米诺定，其次是喷他佐辛≥阿尼利定＞环唑辛=美沙酮＞右丙氧芬≈蒂巴因≥罂粟碱≈阿法罗定＞哌替啶＞吗啡。吗啡的活性为匹米诺定的1%。在相似条件下，匹米诺定比地昔帕明和普罗替林更有效。所研究药物抑制兔血小板摄取间羟胺的效力顺序与用人血小板得到的结果相似。
所研究的镇痛药对单胺摄取抑制作用与其止痛特性不相关。
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