pubmed-article:17260949 | rdf:type | pubmed:Citation | lld:pubmed |
pubmed-article:17260949 | lifeskim:mentions | umls-concept:C0086418 | lld:lifeskim |
pubmed-article:17260949 | lifeskim:mentions | umls-concept:C0035820 | lld:lifeskim |
pubmed-article:17260949 | lifeskim:mentions | umls-concept:C0025914 | lld:lifeskim |
pubmed-article:17260949 | lifeskim:mentions | umls-concept:C0026809 | lld:lifeskim |
pubmed-article:17260949 | lifeskim:mentions | umls-concept:C0036751 | lld:lifeskim |
pubmed-article:17260949 | lifeskim:mentions | umls-concept:C0597357 | lld:lifeskim |
pubmed-article:17260949 | lifeskim:mentions | umls-concept:C0041345 | lld:lifeskim |
pubmed-article:17260949 | lifeskim:mentions | umls-concept:C0443199 | lld:lifeskim |
pubmed-article:17260949 | lifeskim:mentions | umls-concept:C1709915 | lld:lifeskim |
pubmed-article:17260949 | pubmed:issue | 5 | lld:pubmed |
pubmed-article:17260949 | pubmed:dateCreated | 2007-1-30 | lld:pubmed |
pubmed-article:17260949 | pubmed:abstractText | The competitive antagonist d-tubocurarine (curare) has greater potency at mouse than at human 5-hydroxytryptamine 3A (5-HT3A) receptors, despite 84% amino acid sequence identity between the receptors. Within the ligand binding domain of this receptor are six loops (A-F). A previous report demonstrated that loop C of the 5-HT3A receptor contributed to differential potency between the receptors [Hope, A. G. et al. (1999) Mol. Pharmacol. 55, 1037-1043]. The present study tested the hypothesis that loop F plays a significant role in conferring interspecies curare potency differences. Wild-type, chimeric, and point mutant 5-HT3A receptors were expressed in Xenopus oocytes, and two-electrode voltage clamp electrophysiological recordings were performed. Our data suggest that loops C and F contribute to curare potency, given that the curare IC50's (concentration of drug that produces 50% inhibition of the response) for chimeric human receptors with substitutions of mouse residues in loop C (40.07 +/- 2.52 nM) or loop F (131.8 +/- 5.95 nM) were intermediate between those for the mouse (12.99 +/- 0.77 nM) and human (1817 +/- 92.36 nM) wild-type receptors. Two human point mutant receptors containing mouse receptor substitutions in loop F (H-K195E or H-V202I) had significantly lower curare IC50's than that of the human receptor. The human double mutant receptor, H-K195E,V202I, had the same curare IC50 (133.8 +/- 6.38 nM) as that of the human receptor containing all six loop F mouse substitutions. These results demonstrate that two loop F residues make a significant contribution in determining curare potency at the 5-HT3A receptor. | lld:pubmed |
pubmed-article:17260949 | pubmed:grant | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:17260949 | pubmed:language | eng | lld:pubmed |
pubmed-article:17260949 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:17260949 | pubmed:citationSubset | IM | lld:pubmed |
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pubmed-article:17260949 | pubmed:status | MEDLINE | lld:pubmed |
pubmed-article:17260949 | pubmed:month | Feb | lld:pubmed |
pubmed-article:17260949 | pubmed:issn | 0006-2960 | lld:pubmed |
pubmed-article:17260949 | pubmed:author | pubmed-author:GearMM | lld:pubmed |
pubmed-article:17260949 | pubmed:author | pubmed-author:ZhangRanR | lld:pubmed |
pubmed-article:17260949 | pubmed:author | pubmed-author:MachuTina KTK | lld:pubmed |
pubmed-article:17260949 | pubmed:author | pubmed-author:WhiteMichael... | lld:pubmed |
pubmed-article:17260949 | pubmed:author | pubmed-author:LeidenheimerN... | lld:pubmed |
pubmed-article:17260949 | pubmed:author | pubmed-author:HesterBrentB | lld:pubmed |
pubmed-article:17260949 | pubmed:author | pubmed-author:MilitanteJuli... | lld:pubmed |
pubmed-article:17260949 | pubmed:author | pubmed-author:SunHongweiH | lld:pubmed |
pubmed-article:17260949 | pubmed:author | pubmed-author:WenXiaofeiX | lld:pubmed |
pubmed-article:17260949 | pubmed:author | pubmed-author:RhubottomHeat... | lld:pubmed |
pubmed-article:17260949 | pubmed:issnType | Print | lld:pubmed |
pubmed-article:17260949 | pubmed:day | 6 | lld:pubmed |
pubmed-article:17260949 | pubmed:volume | 46 | lld:pubmed |
pubmed-article:17260949 | pubmed:owner | NLM | lld:pubmed |
pubmed-article:17260949 | pubmed:authorsComplete | Y | lld:pubmed |
pubmed-article:17260949 | pubmed:pagination | 1194-204 | lld:pubmed |
pubmed-article:17260949 | pubmed:dateRevised | 2010-11-18 | lld:pubmed |
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pubmed-article:17260949 | pubmed:year | 2007 | lld:pubmed |
pubmed-article:17260949 | pubmed:articleTitle | The role of loop F residues in determining differential d-tubocurarine potencies in mouse and human 5-hydroxytryptamine 3A receptors. | lld:pubmed |
pubmed-article:17260949 | pubmed:affiliation | Department of Pharmacology and Neuroscience, Texas Tech University Health Sciences Center, 3601 Fourth Street, Lubbock, Texas 79430, USA. | lld:pubmed |
pubmed-article:17260949 | pubmed:publicationType | Journal Article | lld:pubmed |
pubmed-article:17260949 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
pubmed-article:17260949 | pubmed:publicationType | Research Support, N.I.H., Extramural | lld:pubmed |
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