Ross S B, Renyi A L
Acta Pharmacol Toxicol (Copenh). 1978 May;42(5):328-36. doi: 10.1111/j.1600-0773.1978.tb02212.x.
The effect of reserpine on the inhibition by (+)-amphetamine and cocaine of the accumulation of 3H-dopamine (DA) in striatal slices and 3H-noradrenaline (NA) in slices of cerebral occipital cortex and heart atrium of rats and the release of 3H-amines from these tissues were examined. Reserpine (5 mg/kg intraperitoneally) was injected 18 hours before the experiments. It was found that reserpine markedly enhanced the in vitro potency of amphetamine in the striatum and heart but only slightly in the cortex. After administration in vivo (+)-amphetamine was about 10 time more potent in reducing the amine accumulation in the cortex as in the striatum. Reserpine enhanced the effect in both regions. The inhibitory potency of cocaine in vitro was unchanged by reserpine in the striatum but was reduced in the cortex and heart. Reserpine did not change the inhibitory potency of desipramine in the cortex and heart. The release of the 3H-amines by (+)-amphetamine was enhanced by reserpine in the striatum and heart but the small release produced in the cortex was not increased. The release produced by cocaine was similarly enhanced by reserpine but cocaine was much less active than (+)-amphetamine. The results indicate that (+)-amphetamine and cocaine inhibit the amine accumulation by different mechanisms.
研究了利血平对(+)-苯丙胺和可卡因抑制大鼠纹状体切片中3H-多巴胺(DA)积累、枕叶皮质切片和心房中3H-去甲肾上腺素(NA)积累以及这些组织中3H-胺释放的影响。实验前18小时腹腔注射利血平(5mg/kg)。结果发现,利血平显著增强了苯丙胺在纹状体和心脏中的体外效力,但在皮质中仅略有增强。体内给药后,(+)-苯丙胺在降低皮质中胺积累方面的效力约为纹状体中的10倍。利血平增强了两个区域的作用。利血平对可卡因在体外抑制纹状体中胺积累的效力无影响,但在皮质和心脏中效力降低。利血平对去甲丙咪嗪在皮质和心脏中的抑制效力无影响。利血平增强了(+)-苯丙胺在纹状体和心脏中释放3H-胺的作用,但在皮质中产生的少量释放未增加。利血平对可卡因产生的释放有类似增强作用,但可卡因的活性远低于(+)-苯丙胺。结果表明,(+)-苯丙胺和可卡因通过不同机制抑制胺积累。