{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,5]],"date-time":"2026-10-05T21:30:49Z","timestamp":1791235849905,"version":"4.1.0"},"reference-count":62,"publisher":"Wiley","issue":"5","license":[{"start":{"date-parts":[[2009,1,30]],"date-time":"2009-01-30T00:00:00Z","timestamp":1233273600000},"content-version":"vor","delay-in-days":1796,"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":[[2004,3]]},"abstract":"<jats:p>\n<jats:list list-type=\"explicit-label\">\n<jats:list-item><jats:p>In order to compare the <jats:italic>\u03b2<\/jats:italic><jats:sub>2<\/jats:sub>\u2010 and <jats:italic>\u03b2<\/jats:italic><jats:sub>3<\/jats:sub>\u2010adrenoceptor (<jats:italic>\u03b2<\/jats:italic>\u2010AR) desensitisation process in human near\u2010term myometrium, we examined the influence of a pretreatment of myometrial strips with either a <jats:italic>\u03b2<\/jats:italic><jats:sub>2<\/jats:sub>\u2010 or a <jats:italic>\u03b2<\/jats:italic><jats:sub>3<\/jats:sub>\u2010AR agonist (salbutamol or SR 59119A, respectively, both at 10 <jats:italic>\u03bc<\/jats:italic><jats:sc>M<\/jats:sc>, for 5 and 15 h) on the relaxation and the cyclic adenosine monophosphate (cAMP) production induced by these agonists.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>To assess some of the mechanisms potentially implicated in the <jats:italic>\u03b2<\/jats:italic>\u2010AR desensitisation process, we studied the influence of such treatment on the number of <jats:italic>\u03b2<\/jats:italic><jats:sub>2<\/jats:sub>\u2010 and <jats:italic>\u03b2<\/jats:italic><jats:sub>3<\/jats:sub>\u2010AR binding sites, the <jats:italic>\u03b2<\/jats:italic><jats:sub>2<\/jats:sub>\u2010 and <jats:italic>\u03b2<\/jats:italic><jats:sub>3<\/jats:sub>\u2010AR transcripts expression and the phosphodiesterase 4 (PDE4) activity.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>Salbutamol, but not SR 59119A, concentration\u2013response curve (CRC) was shifted by a 15 h salbutamol preincubation, with a significant difference in \u2212log EC<jats:sub>20<\/jats:sub> values (6.31\u00b10.13 vs 5.58\u00b10.24, for control and 15 h salbutamol pretreatment, respectively, <jats:italic>P<\/jats:italic>&lt;0.05). Neither salbutamol nor SR 59119A CRCs were modified after a 15 h preincubation with SR 59119A.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>A 15 h exposure of myometrial strips to salbutamol significantly reduced the salbutamol\u2010induced (0.60\u00b10.26 vs 1.54\u00b10.24 pmol mg<jats:sup>\u22121<\/jats:sup> protein, <jats:italic>P<\/jats:italic>&lt;0.05), but not the SR 59119A\u2010induced, cAMP production. No decrease in cAMP production was observed after a 15 h SR 59119A exposure.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>A 15 h salbutamol exposure of myometrial strips significantly reduced the <jats:italic>\u03b2<\/jats:italic><jats:sub>2<\/jats:sub>\u2010 but not the <jats:italic>\u03b2<\/jats:italic><jats:sub>3<\/jats:sub>\u2010AR binding site density, whereas no decrease in the number of <jats:italic>\u03b2<\/jats:italic><jats:sub>2<\/jats:sub>\u2010 and <jats:italic>\u03b2<\/jats:italic><jats:sub>3<\/jats:sub>\u2010AR binding sites was observed after a 15 h SR 59119A treatment.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>Neither PDE4 activity nor the <jats:italic>\u03b2<\/jats:italic><jats:sub>2<\/jats:sub>\u2010 and <jats:italic>\u03b2<\/jats:italic><jats:sub>3<\/jats:sub>\u2010AR mRNA expression levels were affected by salbutamol or SR 59119A treatments.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>Our results indicate that <jats:italic>\u03b2<\/jats:italic><jats:sub>3<\/jats:sub>\u2010AR, but not <jats:italic>\u03b2<\/jats:italic><jats:sub>2<\/jats:sub>\u2010AR, are resistant to the agonist\u2010induced desensitisation. In our model, <jats:italic>\u03b2<\/jats:italic><jats:sub>2<\/jats:sub>\u2010AR desensitisation is mediated by a decreased number of <jats:italic>\u03b2<\/jats:italic><jats:sub>2<\/jats:sub>\u2010AR that was not explained by transcriptional regulation of the receptor.<\/jats:p><\/jats:list-item>\n<\/jats:list>\n<\/jats:p><jats:p><jats:italic>British Journal of Pharmacology<\/jats:italic> (2004) <jats:bold>141<\/jats:bold>, 831\u2013841. doi:<jats:ext-link xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" ext-link-type=\"doi\" xlink:href=\"10.1038\/sj.bjp.0705616\">10.1038\/sj.bjp.0705616<\/jats:ext-link><\/jats:p>","DOI":"10.1038\/sj.bjp.0705616","type":"journal-article","created":{"date-parts":[[2004,3,4]],"date-time":"2004-03-04T20:02:56Z","timestamp":1078430576000},"page":"831-841","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":28,"title":["The human near\u2010term myometrial <i>\u03b2<\/i><sub>3<\/sub>\u2010adrenoceptor but not the <i>\u03b2<\/i><sub>2<\/sub>\u2010adrenoceptor is resistant to desensitisation after sustained agonist stimulation"],"prefix":"10.1111","volume":"141","author":[{"given":"C","family":"Rouget","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"M","family":"Breuiller\u2010Fouch\u00e9","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"F J","family":"Mercier","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"M J","family":"Leroy","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"C","family":"Loustalot","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"E","family":"Naline","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"R","family":"Frydman","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"T","family":"Croci","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"E J","family":"Morcillo","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"C","family":"Advenier","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"M","family":"Bardou","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2009,1,30]]},"reference":[{"key":"e_1_2_7_2_1","doi-asserted-by":"publisher","DOI":"10.1093\/aje\/154.7.657"},{"key":"e_1_2_7_3_1","doi-asserted-by":"publisher","DOI":"10.1159\/000299848"},{"key":"e_1_2_7_4_1","doi-asserted-by":"publisher","DOI":"10.1038\/309163a0"},{"key":"e_1_2_7_5_1","doi-asserted-by":"publisher","DOI":"10.1007\/s002109900092"},{"key":"e_1_2_7_6_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0014-2999(98)00419-1"},{"key":"e_1_2_7_7_1","doi-asserted-by":"publisher","DOI":"10.1038\/sj.bjp.0703491"},{"key":"e_1_2_7_8_1","doi-asserted-by":"publisher","DOI":"10.1016\/0002-9378(83)90682-8"},{"key":"e_1_2_7_9_1","doi-asserted-by":"publisher","DOI":"10.1016\/0002-9378(85)90310-2"},{"key":"e_1_2_7_10_1","doi-asserted-by":"publisher","DOI":"10.1067\/mob.2003.356"},{"key":"e_1_2_7_11_1","doi-asserted-by":"publisher","DOI":"10.1007\/s001090050175"},{"key":"e_1_2_7_12_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1476-5381.1988.tb11698.x"},{"key":"e_1_2_7_13_1","doi-asserted-by":"publisher","DOI":"10.1095\/biolreprod65.2.496"},{"key":"e_1_2_7_14_1","doi-asserted-by":"publisher","DOI":"10.1016\/0003-2697(76)90527-3"},{"key":"e_1_2_7_15_1","doi-asserted-by":"publisher","DOI":"10.1159\/000298771"},{"key":"e_1_2_7_16_1","first-page":"237","article-title":"Desensitization of beta\u20101 and beta\u20102, but not beta\u20103, adrenoceptor\u2010mediated lipolytic responses of adipocytes after long\u2010term norepinephrine infusion","volume":"265","author":"CARPENE C.","year":"1993","journal-title":"J. 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