ANTAGONISM OF L-STEPHOLIDINE ON D2-RECEPTOR-MEDIATED INHIBITION OF SYNAPTOSOMAL ADENYLATE-CYCLASE IN RAT CORPUS STRIATUM
文献类型：期刊论文
| 作者 | HU, G; HU, Y; JIN, GZ
|
| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 1992-03 |
| 卷号 | 13期号:2页码:104-110 |
| 关键词 | BERBINES DOPAMINE RECEPTORS ADENYL CYCLASE GTP PHOSPHOHYDROLASE CORPUS STRIATUM SYNAPTOSOMES |
| ISSN号 | 0253-9756 |
| 文献子类 | Article |
| 英文摘要 | In the presence of Sch 23390 0.1-mu-mol . L-1, dopamine (DA) inhibited the activity of synaptosomal adenylate cyclase (AC) isolated from rat striatum in a concentration-dependent manner with IC50 value of 2.2-mu-mol . L-1. The maximal inhibition corresponded to a 51% decrease of basal enzyme activity and was obtained at DA 100-mu-mol . L-1. The inhibitory effect of DA was reversed by selective D2 receptor antagonist spiperone 10-mu-mol . L-1. N-0437, a selective D2 DA receptor agonist also inhibited the activity of AC in the manner similar to that of DA. Both the inhibitions induced by DA and N-0437 were antagonized by l-stepholidine (l-SPD). However, in the presence of Sch 23390, l-SPD alone also inhibited the activity of AC by 29% and 33% at the concentrations of 10 and 100-mu-mol . L-1, respectively. The inhibition of l-SPD on AC activity was significantly antagonized by spiperone. In the presence of Sch 23390, both DA and N-0437 increased the activity of high affinity GTP phosphohydrolase in striatal synaptosomes. The increases of GTP phosphohydrolase activity stimulated by DA and N-0437 were completely reversed by l-SPD 100-mu-mol . L-1. These results suggest that l-SPD antagonizes or reverses the D2 receptor-mediated inhibition of AC activity through affecting the regulation of G(i) (inhibitory guanine nucleotide-dependent protein) on D2 receptor-coupled AC and therefore affects the negative feedback of presynaptic DA receptors. Moreover, the inhibition of AC activity induced by l-SPD alone may provide a useful biochemical index for dual action of l-SPD. |
| WOS关键词 | TYROSINE-HYDROXYLASE ; RECEPTOR ; GTPASE |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:A1992HH11200002 |
| 出版者 | ACTA PHARMACOLOGICA SINICA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/275169]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | HU, G |
| 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 | HU, G,HU, Y,JIN, GZ. ANTAGONISM OF L-STEPHOLIDINE ON D2-RECEPTOR-MEDIATED INHIBITION OF SYNAPTOSOMAL ADENYLATE-CYCLASE IN RAT CORPUS STRIATUM[J]. ACTA PHARMACOLOGICA SINICA,1992,13(2):104-110. |
| APA | HU, G,HU, Y,&JIN, GZ.(1992).ANTAGONISM OF L-STEPHOLIDINE ON D2-RECEPTOR-MEDIATED INHIBITION OF SYNAPTOSOMAL ADENYLATE-CYCLASE IN RAT CORPUS STRIATUM.ACTA PHARMACOLOGICA SINICA,13(2),104-110. |
| MLA | HU, G,et al."ANTAGONISM OF L-STEPHOLIDINE ON D2-RECEPTOR-MEDIATED INHIBITION OF SYNAPTOSOMAL ADENYLATE-CYCLASE IN RAT CORPUS STRIATUM".ACTA PHARMACOLOGICA SINICA 13.2(1992):104-110. |
入库方式： OAI收割
来源：上海药物研究所
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