{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,10,21]],"date-time":"2025-10-21T14:50:16Z","timestamp":1761058216266},"reference-count":32,"publisher":"Wiley","issue":"8","license":[{"start":{"date-parts":[[2009,2,3]],"date-time":"2009-02-03T00:00:00Z","timestamp":1233619200000},"content-version":"vor","delay-in-days":3839,"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":[[1998,8]]},"abstract":"<jats:p>\n<jats:list list-type=\"explicit-label\">\n<jats:list-item><jats:p>Structure\u2010activity relationships for the binding of human \u03b1\u2010calcitonin gene\u2010related peptide 8\u201337 (h\u03b1CGRP<jats:sub>8\u201337<\/jats:sub>) have been investigated at the CGRP receptors expressed by human SK\u2010N\u2010MC (neuroblastoma) and Col\u200329\u2003(colonic epithelia) cells by radioligand binding assays and functional assays (h\u03b1CGRP stimulation of adenylate cyclase).<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>On SK\u2010N\u2010MC cells the potency order was h\u03b1CGRP<jats:sub>8\u201337<\/jats:sub>&gt;h\u03b1CGRP<jats:sub>19\u201337<\/jats:sub>=AC187&gt;rat amylin<jats:sub>8\u201337<\/jats:sub>&gt; h\u03b1[Tyr<jats:sup>0<\/jats:sup>]\u2010CGRP<jats:sub>28\u201337<\/jats:sub> (apparent pK<jats:sc>B<\/jats:sc>s of 7.49\u00b10.25, 5.89\u00b10.20, 6.18\u00b10.19, 5.85\u00b10.19 and 5.25\u00b10.07). The SK\u2010N\u2010MC receptor appeared CGRP<jats:sub>1<\/jats:sub>\u2010like.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>On Col 29 cells, only h\u03b1CGRP<jats:sub>8\u201337<\/jats:sub> of the above compounds was able to antagonize the actions of h\u03b1CGRP (apparent pK<jats:sc>B<\/jats:sc>=6.48\u00b10.28). Its receptor appeared CGRP<jats:sub>2<\/jats:sub>\u2010like.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>h\u03b1[Ala<jats:sup>11,18<\/jats:sup>]\u2010CGRP<jats:sub>8\u201337<\/jats:sub>, where the amphipathic nature of the N\u2010terminal \u03b1\u2010helix has been reduced, bound to SK\u2010N\u2010MC cells a 100 fold less strongly than h\u03b1CGRP<jats:sub>8\u201337<\/jats:sub>.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>On SK\u2010N\u2010MC cells, h\u03b1CGRP<jats:sub>8\u201318<\/jats:sub>, <jats:sub>28\u201337<\/jats:sub> (M433) and mastoparan\u2010h\u03b1CGRP<jats:sub>28\u201337<\/jats:sub> (M432) had apparent pK<jats:sc>B<\/jats:sc>s of 6.64\u00b10.16 and 6.42\u00b10.26, suggesting that residues 19\u201327 play a minor role in binding. The physico\u2010chemical properties of residues 8\u201318 may be more important than any specific side\u2010chain interactions.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>M433 was almost as potent as h\u03b1CGRP<jats:sub>8\u201337<\/jats:sub> on Col\u200329 cells (apparent pK<jats:sc>B<\/jats:sc>=6.17\u00b10.20). Other antagonists were inactive.<\/jats:p><\/jats:list-item>\n<\/jats:list>\n<\/jats:p><jats:p><jats:italic>British Journal of Pharmacology<\/jats:italic> (1998) <jats:bold>124<\/jats:bold>, 1659\u20131666; doi:<jats:ext-link xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" ext-link-type=\"doi\" xlink:href=\"10.1038\/sj.bjp.0702032\">10.1038\/sj.bjp.0702032<\/jats:ext-link><\/jats:p>","DOI":"10.1038\/sj.bjp.0702032","type":"journal-article","created":{"date-parts":[[2005,1,28]],"date-time":"2005-01-28T19:35:54Z","timestamp":1106940954000},"page":"1659-1666","update-policy":"http:\/\/dx.doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":31,"title":["Structural determinants for binding to CGRP receptors expressed by human SK\u2010N\u2010MC and Col 29 cells: studies with chimeric and other peptides"],"prefix":"10.1111","volume":"124","author":[{"given":"David R","family":"Poyner","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ursel","family":"Soomets","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Stephen G","family":"Howitt","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ulo","family":"Langel","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","first-page":"234P","article-title":"Effect of analogues of CGRP8\u201037 on piglet isolated basilar arteries and 125I\u2010CGRP binding to SK\u2010N\u2010MC cell membranes","volume":"120","author":"Barrett V.J.","year":"1997","journal-title":"Br. 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