Virus R M, Ticho S, Pilditch M, Radulovacki M
Department of Pharmacology, College of Medicine, University of Illinois, Chicago 60612.
Neuropsychopharmacology. 1990 Aug;3(4):243-9.
The dose-response effects of administration of 8-cyclopentyltheophylline (CPT) (10, 20, and 40 mg/kg intraperitoneally [IP]) and alloxazine (ALX) (12.5, 25, and 50 mg/kg, IP) on sleep and wakefulness in rats were examined and compared to those of caffeine (12.5 mg/kg IP). Both CPT and ALX injected individually produced sleep suppression qualitatively similar to that produced by caffeine, but of a lower magnitude. However, when 20 mg/kg CPT and 50 mg/kg ALX were injected together, their sleep suppressant effect was of the same magnitude as that of 12.5 mg/kg caffeine. These results support the hypothesized involvement of adenosine receptor blockade in the effects of caffeine on sleep in rats. They further suggest that A1 adenosine receptor blockade may be more important than A2 receptor blockade, since behavioral effects of the selective in vitro A1 antagonist CPT were generally similar to those of nonselective in vitro adenosine receptor antagonists caffeine and ALX.
研究了腹腔注射8-环戊基茶碱（CPT）（10、20和40mg/kg）和咯嗪（ALX）（12.5、25和50mg/kg）对大鼠睡眠和觉醒的剂量反应效应，并与咖啡因（12.5mg/kg腹腔注射）的效应进行了比较。单独注射CPT和ALX产生的睡眠抑制在性质上与咖啡因产生的相似，但程度较低。然而，当一起注射20mg/kg CPT和50mg/kg ALX时，它们的睡眠抑制作用与12.5mg/kg咖啡因的相同。这些结果支持了腺苷受体阻断参与咖啡因对大鼠睡眠影响的假设。它们进一步表明，A1腺苷受体阻断可能比A2受体阻断更重要，因为选择性体外A1拮抗剂CPT的行为效应通常与非选择性体外腺苷受体拮抗剂咖啡因和ALX的相似。
