CHARACTERIZATION OF 9 SLOWLY DISSOCIATED OPIOID LIGANDS AZABICYCLONONANES COMPOUNDS TO MU, DELTA, AND KAPPA RECEPTORS
文献类型：期刊论文
| 作者 | FAN, LQ; JIN, WQ; CHI, ZQ
|
| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 1991-05 |
| 卷号 | 12期号:3页码:245-249 |
| 关键词 | AZABICYCLONONANES ANALGESICS ENDORPHIN RECEPTORS RADIOLIGAND ASSAY ILEUM VAS DEFERENS |
| ISSN号 | 0253-9756 |
| 文献子类 | Article |
| 英文摘要 | In the receptor binding assay, the relative affinity ratios of P-7548 [3-(beta-phenylethyl)-9-beta-methoxy-9-alpha-(m-propionoxyphenyl)-3-azabicyclo (3,3,1)nonane], P-7556 [3-(beta-phenylethyl)-9-beta-methoxy-9-alpha-(m-benzoyloxyphenyl)-3-azabicyclo(3,3,1)nonane] and P-7618 {3-(beta-phenylethyl)-9-beta-methoxy-9-alpha-[m-(l-cyclopentyl-propionoxyphenyl)]-3-azabicyclo(3,3,1) nonane} were 56:16:1, 1:4:1, and 6:0.2:1 at mu, delta, and kappa-sites, respectively. These compounds possessed a tight binding to mu-receptor. After washed 4 times, they still inhibited the [H-3]ohmefentanyl binding by 70-80%. In the guinea pig ileum, they showed potent and persistent agonist activities, 607, 303, and 181 times respectively that of normorphine. These effects were readily antagonized by naloxone and Mr2266. In the mouse vas deferens (MVD), they also possessed long-lasting agonist activities. The effect of P-7556 on MVD was not antagonized by naloxone and Mr2266, indicating that P-7556 acted on delta-receptor in MVD. In the rabbit vas deferens, P-7548, P-7556, and P-7618 antagonized the effect of U-50488H. We conclude that these azabicyclononanes are a series of opioid ligands with mu, delta-agonist and kappa-antagonist activities. |
| WOS关键词 | ANALGESIC ACTIVITY ; VAS-DEFERENS |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 中文 |
| CSCD记录号 | CSCD:162198 |
| WOS记录号 | WOS:A1991FL66500015 |
| 出版者 | ACTA PHARMACOLOGICA SINICA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/275198]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | FAN, LQ |
| 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 | FAN, LQ,JIN, WQ,CHI, ZQ. CHARACTERIZATION OF 9 SLOWLY DISSOCIATED OPIOID LIGANDS AZABICYCLONONANES COMPOUNDS TO MU, DELTA, AND KAPPA RECEPTORS[J]. ACTA PHARMACOLOGICA SINICA,1991,12(3):245-249. |
| APA | FAN, LQ,JIN, WQ,&CHI, ZQ.(1991).CHARACTERIZATION OF 9 SLOWLY DISSOCIATED OPIOID LIGANDS AZABICYCLONONANES COMPOUNDS TO MU, DELTA, AND KAPPA RECEPTORS.ACTA PHARMACOLOGICA SINICA,12(3),245-249. |
| MLA | FAN, LQ,et al."CHARACTERIZATION OF 9 SLOWLY DISSOCIATED OPIOID LIGANDS AZABICYCLONONANES COMPOUNDS TO MU, DELTA, AND KAPPA RECEPTORS".ACTA PHARMACOLOGICA SINICA 12.3(1991):245-249. |
入库方式： OAI收割
来源：上海药物研究所
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