Involvement of receptor reserve in d-1 agonistic action of (-)-stepholidine in lesioned rats
文献类型：期刊论文
| 作者 | Zou, LL; Liu, JA; Jin, GZ |
| 刊名 | Biochemical pharmacology
 |
| 出版日期 | 1997-07-15 |
| 卷号 | 54期号:2页码:233-240 |
| 关键词 | (-)-stepholidine D-1 dopamine receptor Partial agonist Receptor reserve Adenylate cyclase Rotational behavior |
| ISSN号 | 0006-2952 |
| 英文摘要 | (-)-stepholidine (spd) is a natural produce. previous studies had demonstrated that spd displayed d-1 agonism in unilaterally 6-hydroxydopamine (6-ohda)-lesioned rats and d-1 antagonism in reserpinized rats and normal rats. the aim of the present study was to explain this peculiar pharmacological action based on behavioral and biochemical experiments. in the unilaterally 6-ohda-lesioned rats, spd (4 mg/kg, s.c.) induced contralateral rotation as did apomorphine (apo), but the rotation response to spd was 60% lower than that to apo (0.5 mg/kg, i.p.). coadministration with apo (0.5 mg/kg, i.p.) and spd (0.5 to 10 mg/kg, s.c.) produced a biphasic action curve; at low doses (0.5 or 1 mg/kg), spd potentiated apo action; at high doses (4 or 10 mg/kg), however, spd suppressed apo. in striatal homogenate of the unilaterally lesioned rats, spd stimulated cyclic amp (camp) formation and produced a maximal response comparable to that of dopamine (da) in the denervated striatum, but 70% lower than that of da in the intact striatum. coadministration of 10 mu m da with various concentrations of spd yielded different results, with a biphasic response in the intact side and a synergistic effect in the denervated side. furthermore, based on the determination of receptor mediated camp formation, the d-1 receptor reserve was analyzed in both denervated and intact striatum by using the da receptor inactivator n-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (eedq). the results showed that following eedq administration, the receptor density [revealed by [h-3]r(+)-7-chloro-8-hydroxy-3-methyl 1-phenyl-2,3,4,5-tetrahydro-1h-3-benzazepine ([h-3]sch-23390) binding] and the agonist-stimulated adenylate cyclase (ac) activity (revealed by camp formation) were reduced concur rently. in the intact striatum, the reduction in spd-stimulated ac activity paralleled the receptor loss, indicating the absence of receptor reserve, while in the denervated striatum the reduction in ac activity was less than the receptor loss, indicating a significant level of receptor reserve (estimated 16.4%). by comparison, receptor reserve for da was 45.7 and 25.3% in the denervated and intact striatum, respectively, representing an 80% increase of receptor reserve. in conclusion, spd is a d-1 partial agonist, and receptor reserve permits spd to display its d-1 agonistic action in the unilaterally 6-ohda-lesioned rats. (c) 1997 elsevier science inc. |
| WOS关键词 | TYROSINE-HYDROXYLASE ACTIVITY ; DOPAMINE RECEPTOR ; ADENYLATE-CYCLASE ; CORPUS STRIATUM ; L-STEPHOLIDINE ; TETRAHYDROPROTOBERBERINES ; ANTAGONISTS ; ANALOGS ; INVIVO ; BRAIN |
| WOS研究方向 | Pharmacology & Pharmacy |
| WOS类目 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:A1997XR39600003 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| URI标识 | http://www.irgrid.ac.cn/handle/1471x/2373299 |
| 专题 | 武汉病毒研究所 |
| 作者单位 | CHINESE ACAD SCI,SHANGHAI INST MAT MED,DEPT PHARMACOL,SHANGHAI 200031,PEOPLES R CHINA |
| 推荐引用方式 GB/T 7714 | Zou, LL,Liu, JA,Jin, GZ. Involvement of receptor reserve in d-1 agonistic action of (-)-stepholidine in lesioned rats[J]. Biochemical pharmacology,1997,54(2):233-240. |
| APA | Zou, LL,Liu, JA,&Jin, GZ.(1997).Involvement of receptor reserve in d-1 agonistic action of (-)-stepholidine in lesioned rats.Biochemical pharmacology,54(2),233-240. |
| MLA | Zou, LL,et al."Involvement of receptor reserve in d-1 agonistic action of (-)-stepholidine in lesioned rats".Biochemical pharmacology 54.2(1997):233-240. |
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来源：武汉病毒研究所
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