Source:http://linkedlifedata.com/resource/pubmed/id/14504130
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
5
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| pubmed:dateCreated |
2003-10-30
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| pubmed:abstractText |
Following identification of the human motilin receptor, we isolated the rabbit orthologue by PCR amplification and found this to be 85% identical to the open reading frame of the human receptor. The protein encoded was 84% identical to the human polypeptide. In HEK293T cells transfected with the rabbit receptor, motilin concentration-dependently increased intracellular calcium mobilisation (pEC50=9.25). After transfection with Go1alpha, motilin similarly stimulated [35S]GTPgammaS binding (pEC50=8.87). Using both systems, similar values were obtained with the human receptor, with rank-order potencies of motilin=[Nle13]-motilin>erythromycin; ghrelin was ineffective. In circular muscle preparations of rabbit gastric antrum, [Nle13]-motilin 0.1-30 nM concentration-dependently increased the amplitude of electrically-evoked, neuronally-mediated contractions (pEC50=8.3); higher concentrations increased the muscle tension (30-3000 nM). Both responses to [Nle13]-motilin faded rapidly during its continual presence. Rat or human ghrelin 0.01-10 microM were without activity. Erythromycin 30-3000 nM and 10 microM, respectively, increased neuronal activity and muscle tension in rabbit stomach. Unlike [Nle13]-motilin, the increase in neuronal activity did not fade during continual presence of submaximally-effective concentrations of erythromycin; some fade was observed at higher concentrations. We conclude that the pharmacology of the rabbit motilin receptor is similar to the human orthologue and, when expressed as a recombinant, comparable to the native receptor. However, in terms of their ability to increase neuronal activity in rabbit stomach, [Nle13]-motilin and erythromycin are distinguished by different response kinetics, reflecting different rates of ligand degradation and/or interaction with the receptor.
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| pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/14504130-10081621,
http://linkedlifedata.com/resource/pubmed/commentcorrection/14504130-10381885,
http://linkedlifedata.com/resource/pubmed/commentcorrection/14504130-10754449,
http://linkedlifedata.com/resource/pubmed/commentcorrection/14504130-10764957,
http://linkedlifedata.com/resource/pubmed/commentcorrection/14504130-11159873,
http://linkedlifedata.com/resource/pubmed/commentcorrection/14504130-12032184,
http://linkedlifedata.com/resource/pubmed/commentcorrection/14504130-12054506,
http://linkedlifedata.com/resource/pubmed/commentcorrection/14504130-12522134,
http://linkedlifedata.com/resource/pubmed/commentcorrection/14504130-12606621,
http://linkedlifedata.com/resource/pubmed/commentcorrection/14504130-3786836,
http://linkedlifedata.com/resource/pubmed/commentcorrection/14504130-3797704,
http://linkedlifedata.com/resource/pubmed/commentcorrection/14504130-3843705,
http://linkedlifedata.com/resource/pubmed/commentcorrection/14504130-7935006,
http://linkedlifedata.com/resource/pubmed/commentcorrection/14504130-8495250,
http://linkedlifedata.com/resource/pubmed/commentcorrection/14504130-8804083,
http://linkedlifedata.com/resource/pubmed/commentcorrection/14504130-9088872,
http://linkedlifedata.com/resource/pubmed/commentcorrection/14504130-9430424,
http://linkedlifedata.com/resource/pubmed/commentcorrection/14504130-9863486
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| pubmed:language |
eng
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| pubmed:journal | |
| pubmed:citationSubset |
IM
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| pubmed:chemical | |
| pubmed:status |
MEDLINE
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| pubmed:month |
Nov
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| pubmed:issn |
0007-1188
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| pubmed:author | |
| pubmed:issnType |
Print
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| pubmed:volume |
140
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| pubmed:owner |
NLM
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| pubmed:authorsComplete |
Y
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| pubmed:pagination |
948-54
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| pubmed:dateRevised |
2009-11-18
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| pubmed:meshHeading |
pubmed-meshheading:14504130-Animals,
pubmed-meshheading:14504130-Base Sequence,
pubmed-meshheading:14504130-Cell Line,
pubmed-meshheading:14504130-Dose-Response Relationship, Drug,
pubmed-meshheading:14504130-Humans,
pubmed-meshheading:14504130-Male,
pubmed-meshheading:14504130-Molecular Sequence Data,
pubmed-meshheading:14504130-Motilin,
pubmed-meshheading:14504130-Muscle Contraction,
pubmed-meshheading:14504130-Protein Binding,
pubmed-meshheading:14504130-Pyloric Antrum,
pubmed-meshheading:14504130-Rabbits,
pubmed-meshheading:14504130-Receptors, Gastrointestinal Hormone,
pubmed-meshheading:14504130-Receptors, Neuropeptide
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| pubmed:year |
2003
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| pubmed:articleTitle |
The rabbit motilin receptor: molecular characterisation and pharmacology.
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| pubmed:affiliation |
Department of Gastrointestinal Research, Neurology and Gastroenterology Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. nin_2_dass@gsk.com
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| pubmed:publicationType |
Journal Article,
In Vitro
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