{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,11,11]],"date-time":"2025-11-11T12:41:14Z","timestamp":1762864874700},"reference-count":31,"publisher":"Wiley","issue":"8","license":[{"start":{"date-parts":[[2009,1,29]],"date-time":"2009-01-29T00:00:00Z","timestamp":1233187200000},"content-version":"vor","delay-in-days":3469,"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":[[1999,8]]},"abstract":"<jats:p>\n<jats:list list-type=\"explicit-label\">\n<jats:list-item><jats:p>The newly developed non\u2010peptide neurotensin (NT)\u2010receptor antagonists SR 48692 and SR 142948 were used to challenge NT responses of human colonic circular smooth muscle strips <jats:italic>in vitro<\/jats:italic>. The presence of NT<jats:sub>1<\/jats:sub> and NT<jats:sub>2<\/jats:sub> receptor transcripts in this tissue was tested by reverse transcriptase polymerase chain reaction (RT\u2013PCR) analysis.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>NT potently and dose\u2010dependently contracted muscle strips, with significant regional differences in potency and efficacy between the transverse and distal colon: EC<jats:sub>50<\/jats:sub>, 3.6 and 7.5\u2003n<jats:sc>M<\/jats:sc>; the maximal effect was 70 and 55% of 0.1\u2003m<jats:sc>M<\/jats:sc> carbachol. Colonic responses to NT in both segments were virtually the same in the presence of atropine (1\u2003\u03bc<jats:sc>M<\/jats:sc>), levocabastine (10\u2003\u03bc<jats:sc>M<\/jats:sc>) or tetrodotoxin (1\u2003\u03bc<jats:sc>M<\/jats:sc>).<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>SR 142948 (10\u2003n<jats:sc>M<\/jats:sc>\u20131\u2003\u03bc<jats:sc>M<\/jats:sc>) competitively antagonized NT responses in the transverse and distal colon with similar affinities: pA<jats:sub>2<\/jats:sub> values 8.71 and 8.45, slopes 0.98 and 0.99. SR 48692 (10\u2003n<jats:sc>M<\/jats:sc>\u201310\u2003\u03bc<jats:sc>M<\/jats:sc>) antagonized the NT response competitively in the distal colon (pA<jats:sub>2<\/jats:sub> 6.55, slope 0.79) and non\u2010competitively in the transverse colon (pA<jats:sub>2<\/jats:sub> 8.0, slope 0.51). Neither compound had any agonist effect.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>The fact that the specific antagonists prevented NT\u2010evoked atropine\u2010 and tetrodotoxin\u2010insensitive mechanical responses of colonic muscle strips is highly consistent with the presence in these tissues of non\u2010neuronal NT receptors, whose heterogeneity in the transverse segment is supported by the non\u2010competitive antagonism of SR 48692. The finding of NT<jats:sub>1<\/jats:sub> receptor transcript in both transverse and distal colon suggests its identity with the lower affinity site disclosed functionally by SR 48692 in these segments.<\/jats:p><\/jats:list-item>\n<\/jats:list>\n<\/jats:p><jats:p><jats:italic>British Journal of Pharmacology<\/jats:italic> (1999) <jats:bold>127<\/jats:bold>, 1922\u20131928; doi:<jats:ext-link xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" ext-link-type=\"doi\" xlink:href=\"10.1038\/sj.bjp.0702734\">10.1038\/sj.bjp.0702734<\/jats:ext-link><\/jats:p>","DOI":"10.1038\/sj.bjp.0702734","type":"journal-article","created":{"date-parts":[[2005,1,28]],"date-time":"2005-01-28T20:24:28Z","timestamp":1106943868000},"page":"1922-1928","update-policy":"http:\/\/dx.doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":11,"title":["<i>In vitro<\/i> functional evidence of different neurotensin\u2010receptors modulating the motor response of human colonic muscle strips"],"prefix":"10.1111","volume":"127","author":[{"given":"Tiziano","family":"Croci","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Giulio","family":"Aureggi","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Fabio","family":"Guagnini","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Luciano","family":"Manara","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Danielle","family":"Gully","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"G\u00e9rard","family":"Le Fur","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jean\u2010Pierre","family":"Maffrand","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Sylvain","family":"Mukenge","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Gianfranco","family":"Ferla","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Pascual","family":"Ferrara","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Pascale","family":"Chalon","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Natalio","family":"Vita","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2009,1,29]]},"reference":[{"key":"e_1_2_6_2_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1476-5381.1959.tb00928.x"},{"key":"e_1_2_6_3_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1476-5381.1990.tb14100.x"},{"key":"e_1_2_6_4_1","doi-asserted-by":"publisher","DOI":"10.1016\/0014-5793(96)00397-3"},{"key":"e_1_2_6_5_1","doi-asserted-by":"publisher","DOI":"10.1016\/0003-2697(87)90021-2"},{"key":"e_1_2_6_6_1","doi-asserted-by":"publisher","DOI":"10.1139\/y81-146"},{"key":"e_1_2_6_7_1","first-page":"A176","article-title":"Functional neurotensin and tachykinin NK2\u2010receptors in human strips","volume":"112","author":"CROCI T.","year":"1997","journal-title":"Gastroenterology"},{"key":"e_1_2_6_8_1","doi-asserted-by":"publisher","DOI":"10.1038\/sj.bjp.0701960"},{"key":"e_1_2_6_9_1","doi-asserted-by":"publisher","DOI":"10.1074\/jbc.270.31.18359"},{"key":"e_1_2_6_10_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1476-5381.1994.tb13077.x"},{"key":"e_1_2_6_11_1","doi-asserted-by":"publisher","DOI":"10.1073\/pnas.90.1.65"},{"key":"e_1_2_6_12_1","first-page":"802","article-title":"Biochemical and pharmacological activities of SR 142948A, a new potent neurotensin receptor antagonist","volume":"280","author":"GULLY D.","year":"1997","journal-title":"J. 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