{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,16]],"date-time":"2026-10-16T00:58:53Z","timestamp":1792112333424,"version":"4.4.0"},"reference-count":0,"publisher":"S. Karger AG","license":[{"start":{"date-parts":[[2008,6,10]],"date-time":"2008-06-10T00:00:00Z","timestamp":1213056000000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/karger.com\/pages\/terms-and-conditions"},{"start":{"date-parts":[[2008,6,10]],"date-time":"2008-06-10T00:00:00Z","timestamp":1213056000000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/karger.com\/pages\/terms-and-conditions"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Pharmacology"],"abstract":"<jats:p>Pharmacological and biochemical assays were performed to characterize SR 142801, a new NK-3 receptor antagonist, and its [R]-enantiomer, SR 142806. The compounds were tested (1) in the guinea pig isolated ileum stimulated with [MePhe7]NKB (NK-3 system) in order to evaluate onset and duration of action and to estimate the apparent affinity of the antagonist in terms of pA&lt;sub&gt;2&lt;\/sub&gt; at 140 min after application; (2) in 6 selected monoreceptor systems, the rabbit (rb) vena cava for the NK-lrb receptor, the rabbit pulmonary artery and the hamster (hs) urinary bladder for the NK-2rb and NK-2hs receptors, the rat (r) portal vein for the NK-3r receptor, and in two multireceptor systems adequately treated with NK-1 or NK-2 receptor antagonists to obtain monoreceptor-mediated biological responses (the rat urinary bladder treated with SR 48968 for evaluating the NK-lr and the guinea pig \u2013 gp -ileum treated with CP-99994 for measuring the antagonist affinity on the NK-3gp receptor), in order to evaluate the antagonist selectivity, and (3) in various plasma membrane preparations containing NK-3-binding sites from rats, guinea pigs, and man. The data presented indicate that SR 142801 is a potent, fairly selective non-petide antagonist of the functional (pA&lt;sub&gt;2&lt;\/sub&gt; 9.4) and binding (Ki 0.11 nmol\/l) site of the guinea pig and human (Ki 0.21 nmol\/l) NK-3 receptors, while being much less active on the NK-3 receptors of other species, particularly the rat (pA&lt;sub&gt;2&lt;\/sub&gt; 7.0; Ki 15 nmol\/l). SR 142801 shows a slow onset of action and acts as a long-lasting irreversible antagonist, specific for neurokinin receptors, especially the NK-3 sites of guinea pigs and man.<\/jats:p>","DOI":"10.1159\/000139393","type":"journal-article","created":{"date-parts":[[2008,6,11]],"date-time":"2008-06-11T09:30:10Z","timestamp":1213176610000},"page":"283-291","source":"Crossref","is-referenced-by-count":39,"title":["Pharmacological Characterization of SR 142801: A New Non-Peptide Antagonist of the Neurokinin NK-3 Receptor"],"prefix":"10.1159","author":[{"given":"X.K.","family":"Nguyen-Le","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Q.T.","family":"Nguyen","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"F.","family":"Gobeil","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"L.H.","family":"Pheng","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"X.","family":"Emonds-Alt","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"J.C.","family":"Breli\u00e8re","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"D.","family":"Regoli","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"127","published-online":{"date-parts":[[2008,6,10]]},"container-title":["Pharmacology"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/karger.com\/article-pdf\/doi\/10.1159\/000139393","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2026,5,2]],"date-time":"2026-05-02T16:03:27Z","timestamp":1777737807000},"score":1,"resource":{"primary":{"URL":"https:\/\/karger.com\/article\/doi\/10.1159\/000139393"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2008,6,10]]},"references-count":0,"URL":"https:\/\/doi.org\/10.1159\/000139393","archive":["Portico"],"relation":{},"ISSN":["0031-7012","1423-0313"],"issn-type":[{"value":"0031-7012","type":"print"},{"value":"1423-0313","type":"electronic"}],"subject":[],"published":{"date-parts":[[2008,6,10]]}}}