{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,10,23]],"date-time":"2025-10-23T16:32:51Z","timestamp":1761237171317},"reference-count":53,"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":4112,"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":[[1997,11]]},"abstract":"<jats:p>\n<jats:list list-type=\"explicit-label\">\n<jats:list-item><jats:p>The nature of rat and human fat cell \u03b2<jats:sub>3<\/jats:sub>\u2010adrenoceptors was investigated by studying the effects of the new \u03b2<jats:sub>3<\/jats:sub>\u2010adrenoceptor selective antagonist, SR 59,230A, on lipolysis induced by the conventional \u03b2<jats:sub>3<\/jats:sub>\u2010adrenoceptor agonists, CL 316,243 and SR 58,611A, and by the non\u2010conventional partial \u03b2<jats:sub>3<\/jats:sub>\u2010adrenoceptor agonist CGP 12,177 (a potent \u03b2<jats:sub>1<\/jats:sub>\u2010 and \u03b2<jats:sub>2<\/jats:sub>\u2010adrenoceptor antagonist with partial \u03b2<jats:sub>3<\/jats:sub>\u2010adrenoceptor agonist property).<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>In rat fat cells, the rank order of potency of agonists was: CL 316,243&gt;isoprenaline&gt;SR 58,611A&gt;CGP 12,177. The three former agents were full agonists whereas CGP 12,177 was a partial agonist (intrinsic activity of 0.70). In human fat cells, the lipolytic effect of CGP 12,177 reached 25 % of isoprenaline effect. CL 316,243 was a poor inducer of lipolysis and SR 58,611A was ineffective.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>In rat fat cells, lipolysis induced by CL 316,243 and SR 58,611A was competitively antagonized by SR 59,230A. Schild plots were linear with pA<jats:sub>2<\/jats:sub> values of 6.89 and 6.37, respectively. Conversely, 0.1, 0.5 and 1\u2003\u03bc<jats:sc>M<\/jats:sc> SR 59,230A did not modify the concentration\u2010response curve of CGP 12,177. A rightward shift of the curve was however observed with 10 and 100\u2003\u03bc<jats:sc>M<\/jats:sc> of SR 59,230A. The apparent pA<jats:sub>2<\/jats:sub> value was 5.65. The non\u2010selective \u03b2\u2010adrenergic antagonist, bupranolol, competitively displaced the concentration\u2010response curve of CGP 12,177 and CL 316,243. Schild plots were linear with pA<jats:sub>2<\/jats:sub> values of 6.70 and 7.59, respectively. CL316,243\u2010mediated lipolytic effect was not antagonized by CGP 20,712A. In human fat cells, CGP 12,177\u2010mediated lipolytic effect was antagonized by bupranolol and CGP 20,712A. SR 59,230A (0.1, 1 and 10\u2003\u03bc<jats:sc>M<\/jats:sc>) did not modify the concentration\u2010response curve of CGP 12,177. A rightward shift was however observed at 100\u2003\u03bc<jats:sc>M<\/jats:sc> leading to an apparent pA<jats:sub>2<\/jats:sub> value of 4.32.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>The results suggest that the non\u2010conventional partial agonist CGP 12,177 can activate lipolysis in fat cells through the interaction with a \u03b2\u2010adrenoceptor pharmacologically distinct from the \u03b2<jats:sub>3<\/jats:sub>\u2010adrenoceptor, i.e. through a putative \u03b2<jats:sub>4<\/jats:sub>\u2010adrenoceptor. They suggest that the two subtypes coexist in rat fat cells whereas only the putative \u03b2<jats:sub>4<\/jats:sub>\u2010adrenoceptor mediates lipolytic effect of CGP12,177 in human fat cells.<\/jats:p><\/jats:list-item>\n<\/jats:list>\n<\/jats:p><jats:p><jats:italic>British Journal of Pharmacology<\/jats:italic> (1997) <jats:bold>122<\/jats:bold>, 1244\u20131250; doi:<jats:ext-link xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" ext-link-type=\"doi\" xlink:href=\"10.1038\/sj.bjp.0701523\">10.1038\/sj.bjp.0701523<\/jats:ext-link><\/jats:p>","DOI":"10.1038\/sj.bjp.0701523","type":"journal-article","created":{"date-parts":[[2005,1,28]],"date-time":"2005-01-28T19:17:44Z","timestamp":1106939864000},"page":"1244-1250","update-policy":"http:\/\/dx.doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":63,"title":["Lipolytic effects of conventional <i>\u03b2<\/i><sub>3<\/sub>\u2010adrenoceptor agonists and of CGP 12,177 in rat and human fat cells: preliminary pharmacological evidence for a putative <i>\u03b2<\/i><sub>4<\/sub>\u2010adrenoceptor"],"prefix":"10.1111","volume":"122","author":[{"given":"Jean","family":"Galitzky","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Dominique","family":"Langin","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Patrick","family":"Verwaerde","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jean\u2010Louis","family":"Montastruc","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Max","family":"Lafontan","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Michel","family":"Berlan","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2009,2,3]]},"reference":[{"key":"e_1_2_5_2_1","doi-asserted-by":"publisher","DOI":"10.1002\/med.2610130604"},{"key":"e_1_2_5_3_1","doi-asserted-by":"publisher","DOI":"10.1172\/JCI114880"},{"key":"e_1_2_5_4_1","first-page":"R1729","article-title":"\u03b23\u2010Adrenoceptor in guinea pig brown and white adipocytes: low expression and lack of function","volume":"271","author":"Atgie C.","year":"1996","journal-title":"Am. 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