Tetraethylammonium and 4-aminopyridine enhancement of 5-HT3 receptor-mediated contraction of guinea pig ileum in vitro
文献类型：期刊论文
| 作者 | Yuan, YM; Yang, HH; Hu, GY |
| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 1998-09 |
| 卷号 | 19期号:5页码:451-455 |
| 关键词 | serotonin receptors tetraethylammonium compounds 4-aminopyridine ileum myenteric plexus carbachol serotonin agonists serotonin antagonists radioligand assay |
| ISSN号 | 0253-9756 |
| 文献子类 | Article |
| 英文摘要 | AIM: To study the effects of tetraethylammonium (TEA) and 4-aminopyridine (4-AP) on 5-HT3 receptor-mediated contractions of the isolated guinea pig ileum longitudinal muscle-myenteric plexus strip preparations (GPI). METHODS: GPI contractions were recorded with a chart recorder through isometric transducers. The effect of TEA and 4-AP on binding properties of 5-HT3 receptors was assessed using [H-3]GR65630 binding assay in membrane preparation of rat entorhinal cortex. RESULTS: (1) Both TEA 0.5 mmol . L-1 and 4-AP 5 mu mol . L-1 increased the spontaneous activity, and elicited contractions of GPI; atropine 10 mu mol . L-1 or the selective 5-HT3 receptor antagonist MDL72222 100 mu mol . L-1 prevented these effects. (2) Both TEA 0.05 - 0.5 mmol . L-1 and 4-AP 1-10 mu mol . L-1 enhanced GPI contractions induced by the selective 5-HT3 receptor agonist 2-methyl-5-HT in concentration-dependent manners. (3) Roth TEA 0.5 mmol . L-1 and 4-AP 5 mu mol . L-1 attenuated the inhibitory effects of the selective 5-HT3 receptor antagonists tropisetron 0.1 mu mol . L-1 and benesetron 1 mu mol . L-1 on 5-HT3 receptor-mediated GPI contractions. (4) Neither TEA 0.1 - 0.5 mmol . L-1 nor 4-AP 5 10 mu mol . L-1 affected GPI contractions evoked by the selective M-ACh receptor agonist carbachol 1 mu mol . L-1. (5) TEA 0.5 mmol . L-1 and 4-AP 10 mu mol . L-1 had no effect on the properties of binding of the selective 5-HT3 receptor radioligand [H-3]GR65630 to 5-HT3 receptors. CONCLUSION: The enhancement by TEA and 4-AP of 5-HT3 receptor-mediated GPI contractile responses was due to blocking K+ channels in prejunctional myenteric neurons. |
| WOS关键词 | RELEASE ; ACETYLCHOLINE ; CHANNELS ; CELLS |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000075784800014 |
| 出版者 | ACTA PHARMACOLOGICA SINICA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/274808]  |
| 专题 | 药理学第一研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Hu, GY |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 200031, Peoples R China |
| 推荐引用方式 GB/T 7714 | Yuan, YM,Yang, HH,Hu, GY. Tetraethylammonium and 4-aminopyridine enhancement of 5-HT3 receptor-mediated contraction of guinea pig ileum in vitro[J]. ACTA PHARMACOLOGICA SINICA,1998,19(5):451-455. |
| APA | Yuan, YM,Yang, HH,&Hu, GY.(1998).Tetraethylammonium and 4-aminopyridine enhancement of 5-HT3 receptor-mediated contraction of guinea pig ileum in vitro.ACTA PHARMACOLOGICA SINICA,19(5),451-455. |
| MLA | Yuan, YM,et al."Tetraethylammonium and 4-aminopyridine enhancement of 5-HT3 receptor-mediated contraction of guinea pig ileum in vitro".ACTA PHARMACOLOGICA SINICA 19.5(1998):451-455. |
入库方式： OAI收割
来源：上海药物研究所
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