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

	Chronic treatment with (-)-stepholidine alters density and turnover of D-1 and D-2 receptors in striatum
	Zou, LL; Cai, ST; Jin, GZ
刊名	ACTA PHARMACOLOGICA SINICA
	1996-11
卷号	17 期号:6 页码:485-489
关键词	(-)-stepholidine corpus striatum SCH-23390 radioligand assay dopamine D-1 receptors dopamine D-2 receptors
ISSN号	0253-9756
文献子类	Article
英文摘要	AIM: To study the effects of chronic administration 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-quinoline (EEDQ). RESULTS: Chronic SPD treatment (sc, 20 mg . kg(-1). d(-1) x 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, 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.
WOS关键词	DOPAMINE RECEPTOR ; L-STEPHOLIDINE ; TETRAHYDROPROTOBERBERINES ; SYSTEMS ; RAT
WOS研究方向	Chemistry ; Pharmacology & Pharmacy
语种	英语
CSCD记录号	CSCD:355610
出版者	ACTA PHARMACOLOGICA SINICA
WOS记录号	WOS:A1996VQ48500002
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/274948]
专题	院士及顾问专家
作者单位	CHINESE ACAD SCI,SHANGHAI INST MAT MED,SHANGHAI 200031,PEOPLES R CHINA
推荐引用方式 GB/T 7714	Zou, LL,Cai, ST,Jin, GZ. Chronic treatment with (-)-stepholidine alters density and turnover of D-1 and D-2 receptors in striatum[J]. ACTA PHARMACOLOGICA SINICA,1996,17(6):485-489.
APA	Zou, LL,Cai, ST,&Jin, GZ.(1996).Chronic treatment with (-)-stepholidine alters density and turnover of D-1 and D-2 receptors in striatum.ACTA PHARMACOLOGICA SINICA,17(6),485-489.
MLA	Zou, LL,et al."Chronic treatment with (-)-stepholidine alters density and turnover of D-1 and D-2 receptors in striatum".ACTA PHARMACOLOGICA SINICA 17.6(1996):485-489.