Liu G Q, Algeri S, Garattini S
Arch Int Pharmacodyn Ther. 1982 Jul;258(1):39-50.
D-L-Tetrahydropalmatine (THP), an alkaloid found in the plants of the Carydalis species, has been used as a non-narcotic analgesic and immediate or short-acting hypnotic. The drug's biochemical effects on the rat monoaminergic neuronal system were studied and the findings are presented here. THP's effects on concentrations of dopamine (DA), noradrenaline (NA) and serotonin (5-HT) were determined. In all cases the drug caused a depletion of these transmitters. DA was most markedly affected by treatment (-70%), followed by NA (-50%) and 5-HT (-30%). In parallel with the reduced concentrations of the transmitters there was an increase in their acid and neutral metabolites: HVA and DOPAC for DA, 5HIAA for 5-HT and MHPG-SO4 for NA, indicating that THP increases the release of the monoamines. The concentration of 3-methoxytyramine, an extraneuronal metabolite of DA, was, however, reduced suggesting that the observed increase in metabolism is only an intraneuronal phenomenon and that the release of the neutotransmitter is actually impaired. The effect of THP on the peripheral adrenergic system was also determined. NA stores in heart sympathetic nerves were depleted, but the drug had no effect on the adrenaline content of adrenal glands. The biochemical action of THP seems, therefore, to be similar to that of reserpine-like drugs.
延胡索乙素（THP）是一种存在于紫堇属植物中的生物碱，已被用作非麻醉性镇痛药和速效或短效催眠药。本文研究了该药物对大鼠单胺能神经元系统的生化作用，并展示了研究结果。测定了THP对多巴胺（DA）、去甲肾上腺素（NA）和5-羟色胺（5-HT）浓度的影响。在所有情况下，该药物都会导致这些神经递质的耗竭。DA受治疗的影响最为显著（-70%），其次是NA（-50%）和5-HT（-30%）。随着神经递质浓度的降低，其酸性和中性代谢产物增加：DA的高香草酸（HVA）和3,4-二羟基苯乙酸（DOPAC）、5-HT的5-羟吲哚乙酸（5HIAA）以及NA的3-甲氧基-4-羟基苯乙二醇硫酸酯（MHPG-SO4），这表明THP增加了单胺的释放。然而，DA的一种细胞外代谢产物3-甲氧基酪胺的浓度降低，这表明观察到的代谢增加只是一种细胞内现象，神经递质的释放实际上受到了损害。还测定了THP对外周肾上腺素能系统的影响。心脏交感神经中的NA储备减少，但该药物对肾上腺中的肾上腺素含量没有影响。因此，THP的生化作用似乎与利血平类药物相似。
