慢性给予左旋千金藤立定对纹状体多巴胺D_1和D_2受体密度和更新率的影响  

Chronic treatment with (-) stepholidine alters density and turnover of D 1 and D 2 receptors in striatum 1

作　　者：邹灵龙[1] 蔡舒天 金国章[1] 

机构地区：[1]中国科学院上海药物研究所

出　　处：《中国药理学报》1996年第6期485-489,共5页Acta Pharmacologica Sinica

基　　金：the;National;Natural;Science;Foundation;of;China

摘　　要：慢性给予左旋千金藤立定对纹状体多巴胺Ｄ１和Ｄ２受体密度和更新率的影响１邹灵龙，蔡舒天，金国章２（中国科学院上海药物研究所，上海２０００３１，中国关键词左旋千金藤立定；纹状体；ＳＣＨ２３３９０；放射配位体测定；多巴胺Ｄ１受体；多巴胺Ｄ２受体目的：观察...IM: To study the effects of chronic administra￣tion of SPD on the density and turnover of striatal D 1 and D 2 dopamine (DA) receptors. METHODS: Receptor density was monitored by radio receptor binding assay. The receptor recovery and turnover were studied after irreversible inactivation by N ethoxycarbonyl 2 ethoxy 1,2 dihydro quinol￣ine (EEDQ). RESULTS: Chronic SPD treatment (sc, 20 mg·kg -1 ·d -1 ×21 d) upregulated both striatal D 1 and D 2 receptor density. As compared to vehicle treated rats, SPD increased D 1 and D 2 receptors by 41 5 % and 43 7 %, respectively. SPD also altered the turnover of both D 1 and D 2 receptors. The degradation rate constant ( k =0 0082·h -1 ) and the synthesis rate ( r =2 65 pmol·h -1 /g protein) of D 2 receptors in SPD treated rats were significantly increased vs vehicle treated rats ( k =0 0049·h -1 ; r =1 10 pmol·h -1 /g protein). The degradation rate constant ( k =0 0059·h -1 ) and the synthesis rate ( r =3 1 pmol·h -1 /g protein) of D 1 receptors was also increased in SPD treated rats vs vehicle treated rats ( k =0 0048·h -1 ; r =1 8 pmol·h -1 /g protein), but the alteration of degradation rate constant missed significance ( P >0 05). As a result, receptor recovery following EEDQ was accelerated. The half time for D 1 and D 2 receptors recovery in SPD group were 117 5 h and 84 5 h, respectively, shorter than 144 4 h and 141 4 h in vehicle treated rats. CONCLUSION: Chronic SPD treatment upregulated D 1 and D 2 receptors, and accelerated DA receptor turnover and recovery mainly by increasing receptor synthesis.

关 键 词：左旋千金藤立定 纹状体 放射配位体 多巴胺 受体 

分 类 号：R971[医药卫生—药品] R966[医药卫生—药学]