Airaksinen M M, Lecklin A, Saano V, Tuomisto L, Gynther J
Pharmacol Toxicol. 1987 Jan;60(1):5-8. doi: 10.1111/j.1600-0773.1987.tb01711.x.
The abilities of some naturally occurring beta-carbolines (BCs), dihydro-BCs and tetrahydro-BCs to inhibit the specific binding of 3H-tryptamine (TA), 3H-serotonin (5-HT) and 3H-ketanserine to rat brain membranes and to induce tremor in mice were studied. These compounds, particularly DHBCs and BCs, showed higher affinity for TA binding sites than to 5-HT1 or 5-HT2 binding sites inhibiting the former at nanomolar and the two latter ones at micromolar or high micromolar concentrations. The Ki values for norharmane, harmaline and harmine (17, 18 and 74 nM, respectively) for TA sites indicate the highest affinity so far described for natural beta-carbolines to any receptor sites and thus may indicate their major site of action. among the BC derivatives studied, the before mentioned harmala alkaloids were the most potent inducers of tremor in mice, although the orders of the tremorogenic potency and the binding to TA site did not correlate. It is suggested that especially the tremorigenic effect of BC derivatives is partly based on the binding to specific tryptamine receptors.
研究了一些天然存在的β-咔啉（BCs）、二氢-β-咔啉（DHBCs）和四氢-β-咔啉抑制3H-色胺（TA）、3H-血清素（5-HT）和3H-酮色林与大鼠脑膜特异性结合以及诱导小鼠震颤的能力。这些化合物，尤其是DHBCs和BCs，对TA结合位点的亲和力高于对5-HT1或5-HT2结合位点的亲和力，在纳摩尔浓度下抑制前者，在微摩尔或高微摩尔浓度下抑制后两者。去氢骆驼蓬碱、骆驼蓬碱和骆驼蓬胺对TA位点的Ki值（分别为17、18和74 nM）表明，这是迄今为止所描述的天然β-咔啉对任何受体位点的最高亲和力，因此可能表明它们的主要作用位点。在所研究的BC衍生物中，上述骆驼蓬生物碱是小鼠震颤最有效的诱导剂，尽管震颤诱导效力顺序与与TA位点的结合并不相关。有人提出，特别是BC衍生物的震颤效应部分基于与特定色胺受体的结合。
