| pubmed-article:15806115 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:15806115 | lifeskim:mentions | umls-concept:C0521119 | lld:lifeskim |
| pubmed-article:15806115 | lifeskim:mentions | umls-concept:C0028778 | lld:lifeskim |
| pubmed-article:15806115 | lifeskim:mentions | umls-concept:C1280500 | lld:lifeskim |
| pubmed-article:15806115 | lifeskim:mentions | umls-concept:C1421172 | lld:lifeskim |
| pubmed-article:15806115 | lifeskim:mentions | umls-concept:C0443199 | lld:lifeskim |
| pubmed-article:15806115 | lifeskim:mentions | umls-concept:C0439799 | lld:lifeskim |
| pubmed-article:15806115 | lifeskim:mentions | umls-concept:C0669933 | lld:lifeskim |
| pubmed-article:15806115 | pubmed:issue | 4 | lld:pubmed |
| pubmed-article:15806115 | pubmed:dateCreated | 2005-6-15 | lld:pubmed |
| pubmed-article:15806115 | pubmed:abstractText | 1 2-aminoethoxydiphenyl borate (2-APB) has been widely used to examine the roles of inositol 1,4,5-trisphosphate receptors (IP3Rs) and store-operated Ca2+ entry and is an emerging modulator of cationic channels encoded by transient receptor potential (TRP) genes. 2 Using Ca2+-indicator dye and patch-clamp recording we first examined the blocking effect of 2-APB on human TRPC5 channels expressed in HEK-293 cells. 3 The concentration-response curve has an IC50 of 20 microM and slope close to 1.0, suggesting one 2-APB molecule binds per channel. The blocking effect is not shared by other Ca2+ channel blockers including methoxyverapamil, nifedipine, N-propargylnitrendipine, or berberine. 4 In whole-cell and excised membrane patch recordings, 2-APB acts from the extracellular but not intracellular face of the membrane. 5 Block of TRPC5 by 2-APB is less at positive voltages, suggesting that it enters the electric field or acts by modulating channel gating. 6 2-APB also blocks TRPC6 and TRPM3 expressed in HEK-293 cells, but not TRPM2. 7 Block of TRP channels by 2-APB may be relevant to cell proliferation because 2-APB has a greater inhibitory effect on proliferation in cells overexpressing TRPC5. 8 Our data indicate a specific and functionally important binding site on TRPC5 that enables block by 2-APB. The site is only available via an extracellular route and the block shows mild voltage-dependence. | lld:pubmed |
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| pubmed-article:15806115 | pubmed:language | eng | lld:pubmed |
| pubmed-article:15806115 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15806115 | pubmed:citationSubset | IM | lld:pubmed |
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| pubmed-article:15806115 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:15806115 | pubmed:month | Jun | lld:pubmed |
| pubmed-article:15806115 | pubmed:issn | 0007-1188 | lld:pubmed |
| pubmed-article:15806115 | pubmed:author | pubmed-author:BoulayGuylain... | lld:pubmed |
| pubmed-article:15806115 | pubmed:author | pubmed-author:GrimmChristia... | lld:pubmed |
| pubmed-article:15806115 | pubmed:author | pubmed-author:HarteneckChri... | lld:pubmed |
| pubmed-article:15806115 | pubmed:author | pubmed-author:BeechDavid... | lld:pubmed |
| pubmed-article:15806115 | pubmed:author | pubmed-author:XuShang-Zhong... | lld:pubmed |
| pubmed-article:15806115 | pubmed:author | pubmed-author:ZengFanningF | lld:pubmed |
| pubmed-article:15806115 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:15806115 | pubmed:volume | 145 | lld:pubmed |
| pubmed-article:15806115 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:15806115 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:15806115 | pubmed:pagination | 405-14 | lld:pubmed |
| pubmed-article:15806115 | pubmed:dateRevised | 2009-11-18 | lld:pubmed |
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| pubmed-article:15806115 | pubmed:meshHeading | pubmed-meshheading:15806115... | lld:pubmed |
| pubmed-article:15806115 | pubmed:year | 2005 | lld:pubmed |
| pubmed-article:15806115 | pubmed:articleTitle | Block of TRPC5 channels by 2-aminoethoxydiphenyl borate: a differential, extracellular and voltage-dependent effect. | lld:pubmed |
