Taylor D L, Silverman P B, Ho B T
J Pharm Pharmacol. 1984 Feb;36(2):125-7. doi: 10.1111/j.2042-7158.1984.tb03010.x.
6-MeOTHBC competes for 5-HT binding sites in rat brain in-vitro and in-vivo. The beta-carboline is significantly more active at the type 1 [3H]-5-HT, than the type 2 [3H]spiperone receptors, in-vitro. Following injection, 6-MeOTHBC significantly decreases [3H]-5-HT binding in the cortex. The ineffectiveness on [3H]spiperone binding in-vivo corresponds with the low affinity in-vitro. The effect of 6-MeOTHBC on central 5-HT binding may be a significant aspect of its 5-HT-ergic activity.
6-甲氧基四氢-β-咔啉在体外和体内均能竞争大鼠脑中的5-羟色胺(5-HT)结合位点。在体外,β-咔啉对1型[3H]-5-HT的活性明显高于2型[3H]螺哌隆受体。注射后,6-甲氧基四氢-β-咔啉显著降低皮质中[3H]-5-HT的结合。其对体内[3H]螺哌隆结合无效与体外低亲和力相对应。6-甲氧基四氢-β-咔啉对中枢5-HT结合的影响可能是其5-羟色胺能活性的一个重要方面。