Weir R L, Padgett W, Daly J W, Anderson S M
Epilepsia. 1984 Aug;25(4):492-8. doi: 10.1111/j.1528-1157.1984.tb03449.x.
The anticonvulsant carbamazepine inhibits binding of 1 nM [3H]N6-cyclohexyladenosine to rat cerebral and cerebellar A1 adenosine receptors with an IC50 value of about 50 microM. This concentration is well within that expected for therapeutic regimens. Other anticonvulsants such as phenobarbital, phenytoin, primidone, valproate sodium, and ethosuximide had little or no effect on binding, while theophylline and caffeine caused marked inhibition. Carbamazepine had no marked effect on cyclic AMP levels in guinea pig cerebral cortical or hippocampal slices, but was a weak inhibitor (IC50 about 200 microM) of 2-chloroadenosine-elicited accumulations of cyclic AMP via an A2 adenosine receptor in cortical slices. Carbamazepine is thus a somewhat selective ligand for A1 adenosine receptors in brain. The nature of its activity at those receptors is unclear, but its lack of central stimulant effects contrasts to the stimulant properties of A1 adenosine receptor antagonist such as caffeine and theophylline.
抗惊厥药卡马西平可抑制1 nM [3H]N6-环己基腺苷与大鼠大脑和小脑A1腺苷受体的结合，其半数抑制浓度（IC50）约为50 microM。该浓度完全在治疗方案预期范围内。其他抗惊厥药，如苯巴比妥、苯妥英、扑米酮、丙戊酸钠和乙琥胺，对结合几乎没有影响，而茶碱和咖啡因则引起明显抑制。卡马西平对豚鼠大脑皮质或海马切片中的环磷酸腺苷（cAMP）水平没有明显影响，但在皮质切片中，它是通过A2腺苷受体介导的2-氯腺苷诱导的cAMP积累的弱抑制剂（IC50约为200 microM）。因此，卡马西平是大脑中A1腺苷受体的一种 somewhat selective 配体。其在这些受体上的活性性质尚不清楚，但其缺乏中枢兴奋作用与咖啡因和茶碱等A1腺苷受体拮抗剂的兴奋特性形成对比。
