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Ha, Jeoung-Hee,Shin, Son-Moon,Lee, Soo-Kwan,Kim, Jin-Sook,Shin, Uk-Seob,Huh, Keun,Kim, Jung-Ae,Yong, Chul-Soon,Lee, Nam-Jae,Lee, Dong-Ung 영남대학교 약품개발연구소 2002 영남대학교 약품개발연구소 연구업적집 Vol.11 No.-
The present study was designed to characterize the modulatory effects of the constltuents of Gastrodia elate and their analogues on the GABAergic neurotransmission. 4-Hydroxybenzaldehyde (1) and 4-hydroxy-3-methoxybenzaldehyde (4) inhibited potently the activity of GABA transaminase (IC_50 = 4.1 and 5.4 ㎍/ml,respectively), while the activity of another constituent, 4-hydroxybenzyl alcohol (2), was very weak. Further investigation with 10 analogues revealed a structureactivity correlation, suggesting that the aldehyde group and the hydroxy group at C-4 are necessary for the inhibitory effect on the enzyme activity. Some potent enzyme inhibitors were examined for the effcet on the radioligands to the GABA_A receptor complexes of rat cerebral cortices. Among them, the component 4 dose-dependently lncreased (20-30%) the binding of [^3H]flunitrazepam in the presence of GABA.