Airaksinen M M, Mikkonen E
Med Biol. 1980 Dec;58(6):341-4.
The affinity of beta-carbolines, which may be formed in the body, to benzodiazepine and opiate receptors was studied by measuring their ability to inhibit the binding of [3H]-flunitrazepam and [3H]-dihydromorphine on rat brain synaptosomal membranes. All "aromatized" beta-carbolines studied (norharmane, harmane and 6-methoxyharmane) inhibited the specific binding of [3H]-flunitrazepam in micromolar concentrations, dihydro-beta-carbolines (6-methoxyharmalan, harmalol) were less potent, while all tetrahydro-beta-carbolines showed very low affinity. 6-Hydroxytetrahydroharmane, which is formed by condensation 5HT with acetaldehyde, inhibited [3H]-dihydromorphine binding in micromolar concentration, while norharmane and tetrahydro-beta-carbolines without OH-group showed little affinity. beta-Carbolines are the most potent known natural benzodiazepine receptor ligands. Because they are formed after alcohol drinking, their effects on benzodiazepine and opiate receptors may be connected with alcohol dependence although some beta-carbolines may inhibit 5HT uptake in still lower concentrations.
通过测量β-咔啉（可能在体内形成）对大鼠脑突触体膜上[³H]-氟硝西泮和[³H]-二氢吗啡结合的抑制能力，研究了它们与苯二氮䓬和阿片受体的亲和力。所研究的所有“芳构化”β-咔啉（去甲哈尔满、哈尔满和6-甲氧基哈尔满）在微摩尔浓度下均抑制[³H]-氟硝西泮的特异性结合，二氢-β-咔啉（6-甲氧基二氢哈尔满、去甲骆驼蓬醇）的效力较低，而所有四氢-β-咔啉的亲和力都非常低。由5-羟色胺与乙醛缩合形成的6-羟基四氢哈尔满在微摩尔浓度下抑制[³H]-二氢吗啡的结合，而去甲哈尔满和没有羟基的四氢-β-咔啉的亲和力则很小。β-咔啉是已知最有效的天然苯二氮䓬受体配体。由于它们在饮酒后形成，它们对苯二氮䓬和阿片受体的作用可能与酒精依赖有关，尽管一些β-咔啉在更低浓度下可能抑制5-羟色胺的摄取。
