{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,11,2]],"date-time":"2025-11-02T16:18:13Z","timestamp":1762100293671},"reference-count":47,"publisher":"Wiley","issue":"7","license":[{"start":{"date-parts":[[2009,2,12]],"date-time":"2009-02-12T00:00:00Z","timestamp":1234396800000},"content-version":"vor","delay-in-days":4091,"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":[[1997,12]]},"abstract":"<jats:p>\n<jats:list list-type=\"explicit-label\">\n<jats:list-item><jats:p>This study aimed to investigate the 5\u2010hydroxytryptamine (5\u2010HT) receptors mediating contraction of ring preparations isolated from human pulmonary arteries and veins. In functional studies, the responses to 5\u2010HT, sumatriptan, ergotamine, serotonin\u2010<jats:italic>O<\/jats:italic>\u2010carboxymethyl\u2010glycyl\u2010tyrosinamide (SCMGT), \u03b1\u2010methyl 5\u2010HT (\u03b1\u2010Me) and 2\u2010methyl 5\u2010HT (2\u2010Me) were studied with WAY100635, GR127935, ritanserin, zacopride and SB204070 as antagonists.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>All agonists produced concentration\u2010dependent contractions of human pulmonary artery and vein preparations. The order of potency (\u2212log EC<jats:sub>50<\/jats:sub> values) was ergotamine (6.88)&gt;5\u2010HT (6.41)SCMGT (6.20)=sumatriptan (6.19) \u03b1\u2010Me (6.04) in the artery, and ergotamine (7.84)&gt;5\u2010HT (6.96)&gt;sumatriptan (6.60)=\u03b1\u2010Me (6.56)&gt;SCMGT (6.09) in the vein. The potency of each agonist, except for SCMGT, was greater in vein than in artery preparations. Contractile responses to 5\u2010HT were similar in intact and endothelium\u2010denuded preparations but responses to sumatriptan were enhanced in artery rings without endothelium.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>GR127935 (1\u2003n<jats:sc>M<\/jats:sc> to 0.5\u2003\u03bc<jats:sc>M<\/jats:sc>) produced an unsurmountable antagonism of the response to 5\u2010HT, sumatriptan, ergotamine and SCMGT. Ritanserin (1\u2003n<jats:sc>M<\/jats:sc> to 1\u2003\u03bc<jats:sc>M<\/jats:sc>) also reduced the maximum contractile responses to 5\u2010HT, ergotamine and \u03b1\u2010Me in artery and vein preparations without affecting those to sumatriptan and SCMGT. In endothelium\u2010denuded preparations, surmountable antagonism of sumatriptan by GR127935 (in the presence of ritanserin) and of \u03b1\u2010Me by ritanserin (in the presence of GR127935) allowed for the calculation of the apparent pK<jats:sub>B<\/jats:sub> values of GR127935 (9.17\u00b10.11 in artery and 9.11\u00b10.05 in vein) and ritanserin (8.82\u00b10.09 in artery and 8.98\u00b10.12 in vein).<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>WAY100635 (1\u2003n<jats:sc>M<\/jats:sc> to 1\u2003\u03bc<jats:sc>M<\/jats:sc>), zacopride (1\u2003n<jats:sc>M<\/jats:sc> to 1\u2003\u03bc<jats:sc>M<\/jats:sc>), or SB204070 (1\u2003n<jats:sc>M<\/jats:sc>) did not significantly alter the concentration\u2010response curves for 5\u2010HT, sumatriptan, ergotamine, SCMGT or 2\u2010Me in human pulmonary artery or vein thus indicating that 5\u2010HT<jats:sub>1A<\/jats:sub>, 5\u2010HT<jats:sub>3<\/jats:sub> and 5\u2010HT<jats:sub>4<\/jats:sub> receptors are presumably not involved in the contractile response to these agonists.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>Binding studies using selective radioligands for different 5\u2010HT receptors could not detect the presence of 5\u2010HT<jats:sub>1A<\/jats:sub> receptor binding in human pulmonary blood vessels whereas the 5\u2010HT<jats:sub>1B\/1D<\/jats:sub> radioligand [<jats:sup>3<\/jats:sup>H]\u20105\u2010CT significantly labelled a population of specific binding sites in both vessel types. The presence of 5\u2010HT<jats:sub>2A<\/jats:sub> receptors could also be inferred from the level of binding of [<jats:sup>3<\/jats:sup>H]\u2010ketanserin to membranes obtained from human pulmonary vessels, although significance could not be reached for arteries. 5\u2010HT<jats:sub>4<\/jats:sub> specific receptor binding was scarce in veins and absent in the case of arteries.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>These findings indicate that the human pulmonary artery and vein have a mixed functional population of 5\u2010HT<jats:sub>1B\/1D<\/jats:sub> and 5\u2010HT<jats:sub>2A<\/jats:sub> receptors mediating the contractile response to 5\u2010HT which is consistent with results of the binding studies.<\/jats:p><\/jats:list-item>\n<\/jats:list>\n<\/jats:p>","DOI":"10.1038\/sj.bjp.0701509","type":"journal-article","created":{"date-parts":[[2005,1,28]],"date-time":"2005-01-28T19:18:18Z","timestamp":1106939898000},"page":"1455-1463","update-policy":"http:\/\/dx.doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":47,"title":["Characterization of 5\u2010HT receptors on human pulmonary artery and vein: functional and binding studies"],"prefix":"10.1111","volume":"122","author":[{"given":"Julio","family":"Cortijo","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Miguel","family":"Mart\u00ed\u2010Cabrera","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Eva","family":"Bernabeu","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Teresa","family":"Dom\u00e8nech","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Josep","family":"Bou","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Andr\u00e9s G.","family":"Fern\u00e1ndez","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jorge","family":"Beleta","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jos\u00e9 M.","family":"Palacios","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Esteban J.","family":"Morcillo","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2009,2,12]]},"reference":[{"key":"e_1_2_5_2_1","doi-asserted-by":"publisher","DOI":"10.1016\/0014-2999(92)90488-P"},{"issue":"112","key":"e_1_2_5_3_1","first-page":"1","article-title":"Drug\u2010induced changes of vasomotor tone in isolated human segmental pulmonary arteries","volume":"62","author":"Boe J.","year":"1982","journal-title":"Eur. J. Resp. Dis."},{"key":"e_1_2_5_4_1","first-page":"12","article-title":"Effect of histamine, 5\u2010hydroxytryptamine and prostaglandins on isolated human pulmonary arteries","volume":"61","author":"Boe J.","year":"1980","journal-title":"Eur. J. Resp. Dis."},{"key":"e_1_2_5_5_1","first-page":"1360","article-title":"Pharmacological characterization of serotonin\u2010O\u2010carboxymethyl\u2010glycyl\u2010tyrosinamide, a new selective indolic ligand for 5\u2010hydroxytryptamine (5\u2010HT)1B and (5\u2010HT)1D binding sites","volume":"259","author":"Boulenguez P.","year":"1991","journal-title":"J. Pharmacol. Exp. Ther."},{"key":"e_1_2_5_6_1","doi-asserted-by":"publisher","DOI":"10.1016\/0003-2697(76)90527-3"},{"key":"e_1_2_5_7_1","doi-asserted-by":"publisher","DOI":"10.1136\/hrt.70.6.537"},{"key":"e_1_2_5_8_1","doi-asserted-by":"publisher","DOI":"10.1021\/jm00041a001"},{"key":"e_1_2_5_9_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1476-5381.1989.tb11828.x"},{"key":"e_1_2_5_10_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1476-5381.1986.tb11122.x"},{"key":"e_1_2_5_11_1","doi-asserted-by":"publisher","DOI":"10.1016\/0169-328X(94)90392-1"},{"key":"e_1_2_5_12_1","doi-asserted-by":"publisher","DOI":"10.1007\/PL00005058"},{"key":"e_1_2_5_13_1","first-page":"91P","article-title":"A pharmacological profile of WAY\u2010100635, a potent and selective 5\u2010HT1A receptor antagonist","volume":"112","author":"Fletcher A.","year":"1994","journal-title":"Br. J. Pharmacol."},{"key":"e_1_2_5_14_1","doi-asserted-by":"publisher","DOI":"10.1007\/BF00501438"},{"key":"e_1_2_5_15_1","doi-asserted-by":"publisher","DOI":"10.1038\/305140a0"},{"key":"e_1_2_5_16_1","first-page":"H434","article-title":"Endothelium\u2010dependent relaxation of human pulmonary arteries","volume":"252","author":"Greenberg B.","year":"1987","journal-title":"Am. J. Physiol."},{"key":"e_1_2_5_17_1","doi-asserted-by":"publisher","DOI":"10.1016\/0090-6980(87)90113-4"},{"key":"e_1_2_5_18_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0002-9343(99)80156-9"},{"key":"e_1_2_5_19_1","first-page":"676P","article-title":"The pharmacology of human isolated pulmonary vascular tissues","volume":"47","author":"Houghton J.","year":"1973","journal-title":"Br. J. Pharmacol."},{"key":"e_1_2_5_20_1","doi-asserted-by":"publisher","DOI":"10.3109\/10799898809048978"},{"key":"e_1_2_5_21_1","first-page":"72","volume-title":"The Peripheral Actions of 5\u2010Hydroxytryptamine","author":"Hoyer D.","year":"1989"},{"key":"e_1_2_5_22_1","doi-asserted-by":"publisher","DOI":"10.1016\/0165-6147(93)90129-8"},{"key":"e_1_2_5_23_1","first-page":"157","article-title":"International union of pharmacology classification of receptors for 5\u2010hydroxytryptamine (serotonin)","volume":"46","author":"Hoyer D.","year":"1994","journal-title":"Pharmacol. Rev."},{"key":"e_1_2_5_24_1","doi-asserted-by":"publisher","DOI":"10.1164\/ajrccm\/140.6.1807"},{"key":"e_1_2_5_25_1","doi-asserted-by":"publisher","DOI":"10.1161\/01.CIR.90.3.1141"},{"key":"e_1_2_5_26_1","doi-asserted-by":"publisher","DOI":"10.1006\/pulp.1994.1007"},{"key":"e_1_2_5_27_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1476-5381.1996.tb15982.x"},{"key":"e_1_2_5_28_1","first-page":"1092","article-title":"Adverse reactions to sumatriptan","volume":"341","author":"Maclean M.R.","year":"1993","journal-title":"Lancet"},{"key":"e_1_2_5_29_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1476-5381.1989.tb12033.x"},{"key":"e_1_2_5_30_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1476-5381.1993.tb13750.x"},{"key":"e_1_2_5_31_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1476-5381.1995.tb16627.x"},{"key":"e_1_2_5_32_1","first-page":"762","article-title":"Histamine receptors on human isolated pulmonary arterial muscle preparations: effects of endothelial cell removal and nitric oxide inhibitors","volume":"260","author":"Ortiz J.L.","year":"1992","journal-title":"J. Pharmacol. Exp. Ther."},{"key":"e_1_2_5_33_1","doi-asserted-by":"publisher","DOI":"10.2165\/00023210-199503020-00002"},{"key":"e_1_2_5_34_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1476-5381.1989.tb11835.x"},{"key":"e_1_2_5_35_1","doi-asserted-by":"publisher","DOI":"10.1016\/0028-3908(95)00007-S"},{"key":"e_1_2_5_36_1","doi-asserted-by":"publisher","DOI":"10.1016\/0014-2999(84)90056-6"},{"key":"e_1_2_5_37_1","first-page":"186","article-title":"Response and sensitivity of isolated human pulmonary muscle preparations to pharmacological agents","volume":"233","author":"Raffestin B.","year":"1985","journal-title":"J. Pharmacol. Exp. Ther."},{"key":"e_1_2_5_38_1","doi-asserted-by":"publisher","DOI":"10.1016\/0014-2999(95)00349-P"},{"key":"e_1_2_5_39_1","first-page":"759","article-title":"Biochemical and pharmacological properties of SR 46349B, a new potent and selective 5\u2010hydroxytryptamine2 receptor antagonist","volume":"262","author":"Rinaldi\u2010Carmona M.","year":"1992","journal-title":"J. Pharmacol. Exp. Ther."},{"key":"e_1_2_5_40_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1476-5381.1995.tb17209.x"},{"key":"e_1_2_5_41_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0952-0600(88)80005-X"},{"key":"e_1_2_5_42_1","first-page":"9P","article-title":"GR127935: a potent orally active 5\u2010HT1D receptor antagonist","volume":"110","author":"Skingle M.","year":"1993","journal-title":"Br. J. Pharmacol."},{"key":"e_1_2_5_43_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.2042-7158.1988.tb05253.x"},{"key":"e_1_2_5_44_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1476-5381.1996.tb15555.x"},{"key":"e_1_2_5_45_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1476-5381.1996.tb16700.x"},{"key":"e_1_2_5_46_1","first-page":"299","article-title":"Cumulative dose\u2010response curves. II. Technique for the making of dose\u2013response curves in isolated organs and the evaluation of drug parameters","volume":"143","author":"Rossum J.M.","year":"1963","journal-title":"Arch. Int. Pharmacodyn. Ther."},{"key":"e_1_2_5_47_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1600-0773.1996.tb00179.x"},{"key":"e_1_2_5_48_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1476-5381.1994.tb13148.x"}],"container-title":["British Journal of Pharmacology"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.wiley.com\/onlinelibrary\/tdm\/v1\/articles\/10.1038%2Fsj.bjp.0701509","content-type":"unspecified","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.wiley.com\/onlinelibrary\/tdm\/v1\/articles\/10.1038%2Fsj.bjp.0701509","content-type":"application\/pdf","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/bpspubs.onlinelibrary.wiley.com\/doi\/pdf\/10.1038\/sj.bjp.0701509","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2023,10,27]],"date-time":"2023-10-27T07:32:59Z","timestamp":1698391979000},"score":1,"resource":{"primary":{"URL":"https:\/\/bpspubs.onlinelibrary.wiley.com\/doi\/10.1038\/sj.bjp.0701509"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[1997,12]]},"references-count":47,"journal-issue":{"issue":"7","published-print":{"date-parts":[[1997,12]]}},"alternative-id":["10.1038\/sj.bjp.0701509"],"URL":"https:\/\/doi.org\/10.1038\/sj.bjp.0701509","archive":["Portico"],"relation":{},"ISSN":["0007-1188","1476-5381"],"issn-type":[{"value":"0007-1188","type":"print"},{"value":"1476-5381","type":"electronic"}],"subject":[],"published":{"date-parts":[[1997,12]]},"assertion":[{"value":"2009-02-12","order":2,"name":"published","label":"Published","group":{"name":"publication_history","label":"Publication History"}}]}}