论文部分内容阅读
阐明四氢原小檗碱同类物(THPB)对大鼠中脑腹侧被盖区(VTA)多巴胺(DA)受体的作用特性,并比较它们的作用强度.方法:采用大鼠在体胞外单位放电记录.结果:观察了11个THPB均可完全地翻转DA受体激动剂阿扑吗啡(20μg·kg-1)所产生的放电抑制作用,为D2受体拮抗剂的作用特性.THPB对D2受体的作用与C2位上的OH基团有密切的关系.它们的作用强度(ED50,μg·kg-1):THPB143(56)>SPD(85)>Iso(170)>THP(33)>THB(48)>THPB18(66)>THPB1(179)>THPB19(408)>THPB126(510)>THPB104(1019)>THPB10(4815).结论:11个THPB均为VTAD2受体拮抗剂,以C2位上有OH基团的THPB143作用最强.
To elucidate the effects of tetrahydroprotoberberine (THPB) on dopamine (DA) receptors in the ventral tegular area of rats (VTA) and to compare their effects. Methods: Discharge recorded in extracellular units of rats. RESULTS: Eleven THPBs were able to completely reverse the inhibitory effect of dopamine apomorphine (20 μg · kg -1) on D2 receptor antagonist. The effect of THPB on D2 receptors is closely related to the OH group at C2. (ED50, μg · kg-1): THPB143 (5.6)> SPD (8.5)> Iso (170)> THP (33)> THB (48)> THPB18 (66)> THPB-1 (179)> THPB-19 (408)> THPB-126 (510)> THPB-104 (1019)> THPB-10 (4815). CONCLUSIONS: Eleven THPBs are all VTAD2 receptor antagonists, and THPB-143, which has an OH group on C2 site, has the strongest effect.