| pubmed-article:14654105 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:14654105 | lifeskim:mentions | umls-concept:C0020792 | lld:lifeskim |
| pubmed-article:14654105 | lifeskim:mentions | umls-concept:C0108303 | lld:lifeskim |
| pubmed-article:14654105 | lifeskim:mentions | umls-concept:C1421429 | lld:lifeskim |
| pubmed-article:14654105 | lifeskim:mentions | umls-concept:C1421467 | lld:lifeskim |
| pubmed-article:14654105 | lifeskim:mentions | umls-concept:C0231491 | lld:lifeskim |
| pubmed-article:14654105 | pubmed:issue | 1 | lld:pubmed |
| pubmed-article:14654105 | pubmed:dateCreated | 2003-12-5 | lld:pubmed |
| pubmed-article:14654105 | pubmed:abstractText | Vanilloid receptor-1 (TRPV1) is a non-selective cation channel, predominantly expressed by peripheral sensory neurones, which is known to play a key role in the detection of noxious painful stimuli, such as capsaicin, acid and heat. To date, a number of antagonists have been used to study the physiological role of TRPV1; however, antagonists such as capsazepine are somewhat compromised by non-selective actions at other receptors and apparent modality-specific properties. SB-366791 is a novel, potent, and selective, cinnamide TRPV1 antagonist isolated via high-throughput screening of a large chemical library. In a FLIPR-based Ca(2+)-assay, SB-366791 produced a concentration-dependent inhibition of the response to capsaicin with an apparent pK(b) of 7.74 +/- 0.08. Schild analysis indicated a competitive mechanism of action with a pA2 of 7.71. In electrophysiological experiments, SB-366791 was demonstrated to be an effective antagonist of hTRPV1 when activated by different modalities, such as capsaicin, acid or noxious heat (50 degrees C). Unlike capsazepine, SB-366791 was also an effective antagonist vs. the acid-mediated activation of rTRPV1. With the aim of defining a useful tool compound, we also profiled SB-366791 in a wide range of selectivity assays. SB-366791 had a good selectivity profile exhibiting little or no effect in a panel of 47 binding assays (containing a wide range of G-protein-coupled receptors and ion channels) and a number of electrophysiological assays including hippocampal synaptic transmission and action potential firing of locus coeruleus or dorsal raphe neurones. Furthermore, unlike capsazepine, SB-366791 had no effect on either the hyperpolarisation-activated current (I(h)) or Voltage-gated Ca(2+)-channels (VGCC) in cultured rodent sensory neurones. In summary, SB-366791 is a new TRPV1 antagonist with high potency and an improved selectivity profile with respect to other commonly used TRPV1 antagonists. SB-366791 may therefore prove to be a useful tool to further study the biology of TRPV1. | lld:pubmed |
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| pubmed-article:14654105 | pubmed:language | eng | lld:pubmed |
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| pubmed-article:14654105 | pubmed:citationSubset | IM | lld:pubmed |
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| pubmed-article:14654105 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:14654105 | pubmed:month | Jan | lld:pubmed |
| pubmed-article:14654105 | pubmed:issn | 0028-3908 | lld:pubmed |
| pubmed-article:14654105 | pubmed:author | pubmed-author:DavisJ BJB | lld:pubmed |
| pubmed-article:14654105 | pubmed:author | pubmed-author:SoriaFF | lld:pubmed |
| pubmed-article:14654105 | pubmed:author | pubmed-author:SmartDD | lld:pubmed |
| pubmed-article:14654105 | pubmed:author | pubmed-author:ThompsonMM | lld:pubmed |
| pubmed-article:14654105 | pubmed:author | pubmed-author:OwenDD | lld:pubmed |
| pubmed-article:14654105 | pubmed:author | pubmed-author:EgertonJJ | lld:pubmed |
| pubmed-article:14654105 | pubmed:author | pubmed-author:DaviesC HCH | lld:pubmed |
| pubmed-article:14654105 | pubmed:author | pubmed-author:RandallA DAD | lld:pubmed |
| pubmed-article:14654105 | pubmed:author | pubmed-author:WorbyAA | lld:pubmed |
| pubmed-article:14654105 | pubmed:author | pubmed-author:WymanP APA | lld:pubmed |
| pubmed-article:14654105 | pubmed:author | pubmed-author:RamiH KHK | lld:pubmed |
| pubmed-article:14654105 | pubmed:author | pubmed-author:JermanJ CJC | lld:pubmed |
| pubmed-article:14654105 | pubmed:author | pubmed-author:GillC HCH | lld:pubmed |
| pubmed-article:14654105 | pubmed:author | pubmed-author:GunthorpeM... | lld:pubmed |
| pubmed-article:14654105 | pubmed:author | pubmed-author:NasirSS | lld:pubmed |
| pubmed-article:14654105 | pubmed:author | pubmed-author:SoffinE MEM | lld:pubmed |
| pubmed-article:14654105 | pubmed:author | pubmed-author:Luis HannanSS | lld:pubmed |
| pubmed-article:14654105 | pubmed:author | pubmed-author:LappinS CSC | lld:pubmed |
| pubmed-article:14654105 | pubmed:author | pubmed-author:HowettLL | lld:pubmed |
| pubmed-article:14654105 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:14654105 | pubmed:volume | 46 | lld:pubmed |
| pubmed-article:14654105 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:14654105 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:14654105 | pubmed:pagination | 133-49 | lld:pubmed |
| pubmed-article:14654105 | pubmed:dateRevised | 2010-11-18 | lld:pubmed |
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| pubmed-article:14654105 | pubmed:year | 2004 | lld:pubmed |
| pubmed-article:14654105 | pubmed:articleTitle | Identification and characterisation of SB-366791, a potent and selective vanilloid receptor (VR1/TRPV1) antagonist. | lld:pubmed |
| pubmed-article:14654105 | pubmed:affiliation | Neurology and GI-CEDD, New Frontiers Science Park, GlaxoSmithKline, Harlow, Essex, CM19 5AW, UK. martin_j_gunthorpe@gsk.com | lld:pubmed |
| pubmed-article:14654105 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:14654105 | pubmed:publicationType | Comparative Study | lld:pubmed |
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