{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,7,15]],"date-time":"2025-07-15T03:25:12Z","timestamp":1752549912126},"reference-count":37,"publisher":"Wiley","issue":"6","license":[{"start":{"date-parts":[[2009,2,3]],"date-time":"2009-02-03T00:00:00Z","timestamp":1233619200000},"content-version":"vor","delay-in-days":4357,"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":[[1997,3]]},"abstract":"<jats:p>\n<jats:list list-type=\"explicit-label\">\n<jats:list-item><jats:p>The tachykinin receptors mediating contraction of isolated longitudinal strips of the guinea\u2010pig oesophageal body were characterized with substance P (SP), neurokinin A (NKA) and neurokinin B (NKB) as well as the analogues, [Sar<jats:sup>9<\/jats:sup>,Met(O<jats:sub>2<\/jats:sub>)<jats:sup>11<\/jats:sup>]SP, [Nle<jats:sup>10<\/jats:sup>]NKA(4\u201310) and [MePhe<jats:sup>7<\/jats:sup>]NKB, selective for NK<jats:sub>1<\/jats:sub>, NK<jats:sub>2<\/jats:sub> and NK<jats:sub>3<\/jats:sub>, receptors, respectively. Experiments were performed both in the absence and presence of a cocktail of peptidase inhibitors, captopril (1 \u03bc<jats:sc>m<\/jats:sc>), thiorphan (1 \u03bc<jats:sc>m<\/jats:sc>) and amastatin (20 \u03bc<jats:sc>m<\/jats:sc>), in order to determine whether membrane bound proteases are important in the metabolism of tachykinins in this preparation.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>All agonists produced concentration\u2010dependent contractile effects. The presence of the peptidase inhibitors shifted the concentration\u2010response curves of SP, [Nle<jats:sup>10<\/jats:sup>]NKA(4\u201310) and [MePhe<jats:sup>7<\/jats:sup>]NKB significantly leftwards and the concentration\u2010response curve of NKB was shifted significantly rightwards. However, the EC<jats:sub>50<\/jats:sub> values were significantly different only for [Nle<jats:sup>10<\/jats:sup>]NKA(4\u201310) and NKB.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>In the presence of the peptidase inhibitors, the EC<jats:sub>50<\/jats:sub> values of the selective agonists, [MePhe<jats:sup>7<\/jats:sup>]NKB (0.6 n<jats:sc>m<\/jats:sc>) and [Nle<jats:sup>10<\/jats:sup>]NKA(4\u201310) (66 n<jats:sc>m<\/jats:sc>) indicated the presence of both tachykinin NK<jats:sub>3<\/jats:sub> and NK<jats:sub>2<\/jats:sub> receptors. [MePhe<jats:sup>7<\/jats:sup>]NKB produced less than 50% of the maximal response obtained with the other agonists. Since [Sar<jats:sup>9<\/jats:sup>,Met(O<jats:sub>2<\/jats:sub>)<jats:sup>11<\/jats:sup>]SP produced a small response in the nanomolar concentration range in about 30% of the preparations tested, it is possible that some NK<jats:sub>1<\/jats:sub> receptors were also present.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>Assuming competitive antagonism, the NK<jats:sub>2<\/jats:sub>\u2010selective antagonist SR 48,968 (30 n<jats:sc>m<\/jats:sc>) gave apparent p<jats:italic>K<\/jats:italic><jats:sub>B<\/jats:sub> values of 8.13 and 8.65 for [Nle<jats:sup>10<\/jats:sup>]NKA(4\u201310) in the absence and presence of peptidase inhibitors, respectively, supporting the presence of NK<jats:sub>2<\/jats:sub> receptors.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>The NK<jats:sub>3<\/jats:sub>\u2010selective antagonist SR 142,801 (0.1 \u03bc<jats:sc>m<\/jats:sc>), suppressed responses to low (0.1\u201310 n<jats:sc>m<\/jats:sc>) concentrations of [MePhe<jats:sup>7<\/jats:sup>]NKB. These contractile responses to [MePhe<jats:sup>7<\/jats:sup>]NKB were also abolished by atropine (0.6 \u03bc<jats:sc>m<\/jats:sc>) suggesting that this response was mediated via cholinergic nerves.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>It is concluded that the guinea\u2010pig oesophagus is a complex system which has both NK<jats:sub>2<\/jats:sub> and NK<jats:sub>3<\/jats:sub> receptors and possibly some NK<jats:sub>1<\/jats:sub> receptors as well.<\/jats:p><\/jats:list-item>\n<\/jats:list>\n<\/jats:p><jats:p><jats:italic>British Journal of Pharmacology<\/jats:italic> (1997) <jats:bold>120<\/jats:bold>, 1021\u20131028; doi:<jats:ext-link xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" ext-link-type=\"doi\" xlink:href=\"10.1038\/sj.bjp.0701001\">10.1038\/sj.bjp.0701001<\/jats:ext-link><\/jats:p>","DOI":"10.1038\/sj.bjp.0701001","type":"journal-article","created":{"date-parts":[[2006,8,25]],"date-time":"2006-08-25T16:12:00Z","timestamp":1156522320000},"page":"1021-1028","update-policy":"http:\/\/dx.doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":9,"title":["Tachykinin receptors in the guinea\u2010pig isolated oesophagus: a complex system"],"prefix":"10.1111","volume":"120","author":[{"given":"K P","family":"Kerr","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"F","family":"Mitchelson","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"I M","family":"Coupar","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2009,2,3]]},"reference":[{"key":"e_1_2_6_2_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0006-291X(05)80041-5"},{"key":"e_1_2_6_3_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1476-5381.1959.tb00928.x"},{"key":"e_1_2_6_4_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1476-5381.1994.tb14775.x"},{"key":"e_1_2_6_5_1","doi-asserted-by":"publisher","DOI":"10.1016\/0166-2236(94)90149-X"},{"key":"e_1_2_6_6_1","doi-asserted-by":"publisher","DOI":"10.1016\/0016-5085(78)90416-X"},{"key":"e_1_2_6_7_1","doi-asserted-by":"publisher","DOI":"10.1172\/JCI109667"},{"key":"e_1_2_6_8_1","doi-asserted-by":"publisher","DOI":"10.1016\/0143-4179(87)90088-6"},{"key":"e_1_2_6_9_1","doi-asserted-by":"publisher","DOI":"10.1016\/0024-3205(94)00413-M"},{"key":"e_1_2_6_10_1","doi-asserted-by":"publisher","DOI":"10.1016\/0014-2999(93)90027-F"},{"key":"e_1_2_6_11_1","doi-asserted-by":"publisher","DOI":"10.1016\/0024-3205(92)90352-P"},{"key":"e_1_2_6_12_1","first-page":"590","article-title":"Characterization of the tachykinin neurokinin\u20102 receptor in the human urinary bladder by means of selective receptor antagonists and peptidase inhibitors","volume":"267","author":"Giuliani S.","year":"1993","journal-title":"J. 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