| pubmed-article:9098692 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:9098692 | lifeskim:mentions | umls-concept:C0295352 | lld:lifeskim |
| pubmed-article:9098692 | lifeskim:mentions | umls-concept:C1522642 | lld:lifeskim |
| pubmed-article:9098692 | lifeskim:mentions | umls-concept:C0243192 | lld:lifeskim |
| pubmed-article:9098692 | lifeskim:mentions | umls-concept:C0231491 | lld:lifeskim |
| pubmed-article:9098692 | lifeskim:mentions | umls-concept:C0728938 | lld:lifeskim |
| pubmed-article:9098692 | lifeskim:mentions | umls-concept:C0302891 | lld:lifeskim |
| pubmed-article:9098692 | pubmed:issue | 2-3 | lld:pubmed |
| pubmed-article:9098692 | pubmed:dateCreated | 1997-6-16 | lld:pubmed |
| pubmed-article:9098692 | pubmed:abstractText | Effects of (R)-N-(quinuclidin-3-yl)-2-(1-methyl-1 H-indol-3-yl)-2-oxo-acetamide (RS-056812-198) on 5-HT3 receptors have been investigated in whole-cell voltage-clamped N1E-115 mouse neuroblastoma cells and on 5-HT3 receptors composed of either long (5-HT3R-Al) or short (5-HT3R-AS) subunits expressed in Xenopus laevis oocytes. In N1E-115 cells RS-056812-198 evokes small transient inward currents, which are completely and reversibly inhibited by the selective 5-HT3 receptor antagonist MDL 72222 and cross-desensitizes with the 5-hydroxytryptamine (5-HT)-evoked current. The concentration-effect curve of RS-056812-198 yields an EC50 of 18 nM and a maximum amplitude of 15% of the maximum 5-HT-evoked current. In contrast to its effects on N1E-115 cells, RS-056812-198 does not evoke an ion current on cloned 5-HT3 receptors expressed in Xenopus oocytes, but acts as an antagonist. For 5-HT3R-A1 receptors, the IC50 of RS-056812-198 is 0.4 nM. The results show that (I) RS-056812-198 is a high-affinity partial agonist on 5-HT3 receptors in N1E-115 cells, thus providing a valuable tool to study agonist-receptor interaction in more detail: (2) 5-HT3 receptors on N1E-115 cells differ from the homo-oligomeric 5-HT3 receptors expressed in Xenopus oocytes. Whether the difference is caused by differences in protein processing in the two preparations or by expression of additional, yet unidentified subunits in N1E-115 cells and consequent formation of hetero-oligomeric 5-HT3 receptors remains to be determined. | lld:pubmed |
| pubmed-article:9098692 | pubmed:language | eng | lld:pubmed |
| pubmed-article:9098692 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:9098692 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:9098692 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:9098692 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:9098692 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:9098692 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:9098692 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:9098692 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:9098692 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:9098692 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:9098692 | pubmed:month | Mar | lld:pubmed |
| pubmed-article:9098692 | pubmed:issn | 0014-2999 | lld:pubmed |
| pubmed-article:9098692 | pubmed:author | pubmed-author:VijverbergH... | lld:pubmed |
| pubmed-article:9098692 | pubmed:author | pubmed-author:Van HooftJ... | lld:pubmed |
| pubmed-article:9098692 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:9098692 | pubmed:day | 19 | lld:pubmed |
| pubmed-article:9098692 | pubmed:volume | 322 | lld:pubmed |
| pubmed-article:9098692 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:9098692 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:9098692 | pubmed:pagination | 229-33 | lld:pubmed |
| pubmed-article:9098692 | pubmed:dateRevised | 2010-11-18 | lld:pubmed |
| pubmed-article:9098692 | pubmed:meshHeading | pubmed-meshheading:9098692-... | lld:pubmed |
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| pubmed-article:9098692 | pubmed:meshHeading | pubmed-meshheading:9098692-... | lld:pubmed |
| pubmed-article:9098692 | pubmed:meshHeading | pubmed-meshheading:9098692-... | lld:pubmed |
| pubmed-article:9098692 | pubmed:meshHeading | pubmed-meshheading:9098692-... | lld:pubmed |
| pubmed-article:9098692 | pubmed:meshHeading | pubmed-meshheading:9098692-... | lld:pubmed |
| pubmed-article:9098692 | pubmed:meshHeading | pubmed-meshheading:9098692-... | lld:pubmed |
| pubmed-article:9098692 | pubmed:meshHeading | pubmed-meshheading:9098692-... | lld:pubmed |
| pubmed-article:9098692 | pubmed:meshHeading | pubmed-meshheading:9098692-... | lld:pubmed |
| pubmed-article:9098692 | pubmed:year | 1997 | lld:pubmed |
| pubmed-article:9098692 | pubmed:articleTitle | RS-056812-198: partial agonist on native and antagonist on cloned 5-HT3 receptors. | lld:pubmed |
| pubmed-article:9098692 | pubmed:affiliation | Research Institute of Toxicology, Utrecht University, Netherlands. h.vanhooft@ritox.dgk.ruu.nl | lld:pubmed |
| pubmed-article:9098692 | pubmed:publicationType | Journal Article | lld:pubmed |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:9098692 | lld:pubmed |
