Wauquier A, Van Belle H, Van den Broeck W A, Janssen P A
Psychopharmacology (Berl). 1987;91(4):434-9. doi: 10.1007/BF00216007.
Mioflazine, a nucleoside transport inhibitor, was given PO to dogs at doses of 0.04-10 mg/kg. Sixteen hour polygraphic sleep recordings were made and analysis and sleep stage classification was done by computer. Mioflazine decreased wakefulness and increased slow wave sleep, but did not affect the latencies of either REM sleep or slow wave sleep. This increased sleep was due to an increase in the number of light and deep slow wave sleep epochs. The effect lasted for about 8 h. The decreased wakefulness and increased slow wave sleep could be antagonized by the adenosine antagonist caffeine (2.5 and 10 mg/kg, PO); however, there was not a pure antagonistic effect. It might be that the enhancement of slow wave sleep is due to an activation of brain adenosine receptors. This is the first report of a drug acting on adenosine that given orally improves sleep. Mioflazine might be the prototype of substances worth considering for the treatment of a variety of sleep disorders.
米诺嗪是一种核苷转运抑制剂，以0.04 - 10毫克/千克的剂量口服给予犬类。进行了16小时的多导睡眠记录，并通过计算机进行分析和睡眠阶段分类。米诺嗪减少了清醒时间，增加了慢波睡眠，但不影响快速眼动睡眠或慢波睡眠的潜伏期。睡眠增加是由于浅睡眠和深睡眠慢波睡眠时段数量增加。这种效果持续约8小时。清醒时间的减少和慢波睡眠的增加可被腺苷拮抗剂咖啡因（2.5和10毫克/千克，口服）拮抗；然而，并非完全拮抗作用。慢波睡眠增强可能是由于脑腺苷受体的激活。这是关于一种作用于腺苷的药物口服改善睡眠的首次报道。米诺嗪可能是值得考虑用于治疗各种睡眠障碍的物质原型。
