Partial agonistic effect of yokukansan on human recombinant serotonin 1A receptors expressed in the membranes of Chinese hamster ovary cells

摘要: Abstract Ethnopharmacological relevance Yokukansan (YKS) is a traditional Japanese medicine consisted of seven medicinal herbs and has been used for treatment neurosis, insomnia, behavioral psychological symptoms dementia (BPSD) in Japan. Aim the study The aim present to clarify intrinsic activity YKS on serotonin (5-HT)1A 5-HT2A receptors also determine constituent which are responsible effect YKS. Materials methods dry powdered extracts YKS, herbs, YKS-analogues were produced by eliminating one from manufacturing process, evaluation. Competitive binding assays 5-HT [ 35 S]GTPγS evaluation agonistic/antagonistic performed using Chinese hamster ovary cell membranes stably expressing human recombinant 5-HT1A or receptors. Results (6.25–400 μg/ml) concentration-dependently inhibited 3 H]8-OH-DPAT IC 50 value was estimated be 61.2 μg/ml. In contrast, failed inhibit H]ketanserin Only Uncaria hook (3.13–50 μg/ml), herbal extracts, concentration-dependent manner, 7.42 μg/ml. increased approximately 50% that full agonist, 5-HT. Both competitive remarkably attenuated but it almost unchanged when other eliminated Conclusion These results suggest partial agonistic receptors, mainly attributed hook.