{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,1,13]],"date-time":"2026-01-13T15:30:48Z","timestamp":1768318248312,"version":"3.49.0"},"reference-count":24,"publisher":"Wiley","issue":"5","license":[{"start":{"date-parts":[[2009,2,2]],"date-time":"2009-02-02T00:00:00Z","timestamp":1233532800000},"content-version":"vor","delay-in-days":1920,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"content-domain":{"domain":["bpspubs.onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["British J Pharmacology"],"published-print":{"date-parts":[[2003,11]]},"abstract":"<jats:p>\n<jats:list list-type=\"explicit-label\">\n<jats:list-item><jats:p>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.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>In HEK293T cells transfected with the rabbit receptor, motilin concentration\u2010dependently increased intracellular calcium mobilisation (<jats:italic>p<\/jats:italic>EC<jats:sub>50<\/jats:sub>=9.25). After transfection with G<jats:sub>o1<\/jats:sub><jats:italic>\u03b1<\/jats:italic>, motilin similarly stimulated [<jats:sup>35<\/jats:sup>S]GTP<jats:italic>\u03b3<\/jats:italic>S binding (<jats:italic>p<\/jats:italic>EC<jats:sub>50<\/jats:sub>=8.87). Using both systems, similar values were obtained with the human receptor, with rank\u2010order potencies of motilin=[Nle<jats:sup>13<\/jats:sup>]\u2010motilin&gt;erythromycin; ghrelin was ineffective.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>In circular muscle preparations of rabbit gastric antrum, [Nle<jats:sup>13<\/jats:sup>]\u2010motilin 0.1\u201330 n<jats:sc>M<\/jats:sc> concentration\u2010dependently increased the amplitude of electrically\u2010evoked, neuronally\u2010mediated contractions (<jats:italic>p<\/jats:italic>EC<jats:sub>50<\/jats:sub>=8.3); higher concentrations increased the muscle tension (30\u20133000 n<jats:sc>M<\/jats:sc>). Both responses to [Nle<jats:sup>13<\/jats:sup>]\u2010motilin faded rapidly during its continual presence. Rat or human ghrelin 0.01\u201310 <jats:italic>\u03bc<\/jats:italic><jats:sc>M<\/jats:sc> were without activity.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>Erythromycin 30\u20133000 n<jats:sc>M<\/jats:sc> and 10 <jats:italic>\u03bc<\/jats:italic><jats:sc>M<\/jats:sc>, respectively, increased neuronal activity and muscle tension in rabbit stomach. Unlike [Nle<jats:sup>13<\/jats:sup>]\u2010motilin, the increase in neuronal activity did not fade during continual presence of submaximally\u2010effective concentrations of erythromycin; some fade was observed at higher concentrations.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>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, [Nle<jats:sup>13<\/jats:sup>]\u2010motilin and erythromycin are distinguished by different response kinetics, reflecting different rates of ligand degradation and\/or interaction with the receptor.<\/jats:p><\/jats:list-item>\n<\/jats:list>\n<\/jats:p><jats:p><jats:italic>British Journal of Pharmacology<\/jats:italic> (2003) <jats:bold>140<\/jats:bold>, 948\u2013954. doi:<jats:ext-link xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" ext-link-type=\"doi\" xlink:href=\"10.1038\/sj.bjp.0705505\">10.1038\/sj.bjp.0705505<\/jats:ext-link><\/jats:p>","DOI":"10.1038\/sj.bjp.0705505","type":"journal-article","created":{"date-parts":[[2003,10,29]],"date-time":"2003-10-29T21:07:59Z","timestamp":1067461679000},"page":"948-954","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":68,"title":["The rabbit motilin receptor: molecular characterisation and pharmacology"],"prefix":"10.1111","volume":"140","author":[{"given":"N B","family":"Dass","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"J","family":"Hill","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"A","family":"Muir","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"T","family":"Testa","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"A","family":"Wise","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"G J","family":"Sanger","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2009,2,2]]},"reference":[{"key":"e_1_2_7_2_1","doi-asserted-by":"publisher","DOI":"10.1053\/gast.2001.22158"},{"key":"e_1_2_7_3_1","first-page":"243","article-title":"Discovery of the first non\u2010peptide antagonist of the motilin receptor","volume":"17","author":"BEAVERS M.P.","year":"2001","journal-title":"Drug Design Discov."},{"key":"e_1_2_7_4_1","doi-asserted-by":"publisher","DOI":"10.1016\/0167-0115(86)90084-4"},{"key":"e_1_2_7_5_1","doi-asserted-by":"publisher","DOI":"10.1046\/j.1440-1681.1999.03022.x"},{"key":"e_1_2_7_6_1","doi-asserted-by":"publisher","DOI":"10.1136\/gut.43.3.395"},{"key":"e_1_2_7_7_1","doi-asserted-by":"publisher","DOI":"10.1124\/jpet.102.047563"},{"key":"e_1_2_7_8_1","doi-asserted-by":"publisher","DOI":"10.1126\/science.284.5423.2184"},{"issue":"1","key":"e_1_2_7_9_1","article-title":"Molecular, functional and cross\u2010species comparisons between the receptors for the prokinetic neuropeptides, motilin and ghrelin","volume":"122","author":"HILL J.","year":"2002","journal-title":"Gastroenterology"},{"key":"e_1_2_7_10_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1476-5381.1993.tb13536.x"},{"key":"e_1_2_7_11_1","doi-asserted-by":"publisher","DOI":"10.1152\/ajpgi.2000.278.1.G18"},{"key":"e_1_2_7_12_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0196-9781(99)00198-9"},{"key":"e_1_2_7_13_1","first-page":"G418","article-title":"Gastrokinetic effects of erythromycin \u2013 myogenic and neurogenic mechanisms of action in rabbit stomach","volume":"32","author":"PARKMAN H.P.","year":"1995","journal-title":"Am. 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