1-Stepholidine,Adenosine A2A Receptor and Dopamine D3 Receptor Interactions
会议名称：《第十五届国际药理学大会》
会议日期：2006年
学科分类：1001[医学-基础医学(可授医学、理学学位)] 10[医学]
基 金：Project supperted by the Ministry of Science and Technology (973-2003CB515401) the National Natural Science Foundation of China (No 30271495,No 30472009)
关 键 词：1 - Stepholidine dopamine D3 receptor adenosine A2a receptor
摘 要：正 Aim: 1 - Stepholidine （SPD） is a lead compound of tetrahydroprotoberberines （THPBs）. This work investigated the influence of SPD on Dopamine D3 receptor （D3R） and adenosine A2a receptor （A2aR）. Methods: PC12 cells with endogenous A2aR were transfected with pIRES - D3R plasmids by Lipofectamine?2000 transfection kit. Protein expression was assessed by Western blot. mRNA was detected by Real - time polymerase chain reaction. The accumulation of cyclic AMP from cells was measured by HitHunter cAMP II Assay kit. Results: Incubation of PC12 cells expressed D3R with SPD resulted in a little decrease of D3 receptors in protein expression. SPD can decrease of D3R and A2aR mRNA level in PC12 cells which stably expressed D3R. SPD or D3 receptor agonist counteracted the A2aR receptor agonist - mediated increase in cAMP levels. Blockade of D3R with the D3R antagonist increased both basal and A2aR receptor agonist - stimulated cAMP levels. Conclusion: These results suggest SPD is a agonist for D3R stably expressed in PC12 cells. The D3R can modulate A2a receptors at the level of gene transcription and the generation of second messengers.