{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,9,10]],"date-time":"2025-09-10T23:32:12Z","timestamp":1757547132485},"reference-count":0,"publisher":"Canadian Science Publishing","issue":"1","license":[{"start":{"date-parts":[[1987,1,1]],"date-time":"1987-01-01T00:00:00Z","timestamp":536457600000},"content-version":"tdm","delay-in-days":0,"URL":"http:\/\/www.nrcresearchpress.com\/page\/about\/CorporateTextAndDataMining"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Can. J. Physiol. Pharmacol."],"published-print":{"date-parts":[[1987,1,1]]},"abstract":"<jats:p> Interactions of derivatives of befunolol (BFE-37, BFE-55, and BFE-61), carteolol, and pindolol with \u03b2-adrenoceptors were tested in guinea pig isolated taenia caecum. All the drugs used acted as partial agonists on the \u03b2-adrenoceptors when compared with isoprenaline, a full agonist. The pA<jats:sub>2<\/jats:sub> values of BFE-61, carteolol, and pindolol were significantly larger than their pD<jats:sub>2<\/jats:sub> values, while there was no significant difference between the pA<jats:sub>2<\/jats:sub> and pD<jats:sub>2<\/jats:sub> values for BFE-37 and BFE-55. The specific binding of [<jats:sup>3<\/jats:sup>H]befunolol to microsomal fractions from the guinea pig taenia caecum distinguished two binding sites, high affinity and low affinity sites. Both sites are considered to be bound by 50\u2002nM of [<jats:sup>3<\/jats:sup>H]befunolol. Specific <jats:sup>3<\/jats:sup>H binding was displaced by BFE-61, carteolol, and pindolol in a biphasic manner but in a monophasic manner by BFE-37 and BFE-55. Furthermore, [<jats:sup>3<\/jats:sup>H]befunolol binding was only partially displaced by BFE-55 but completely displaced by the other drugs used. These results, together with our previous findings, suggest that BFE-61, carteolol, and pindolol discriminate between the two affinity binding sites in the \u03b2-adrenoceptors, which are not discriminated between by BFE-37, and further that BFE-55 may bind with only the high affinity site. <\/jats:p>","DOI":"10.1139\/y87-004","type":"journal-article","created":{"date-parts":[[2011,4,24]],"date-time":"2011-04-24T04:54:33Z","timestamp":1303620873000},"page":"18-22","source":"Crossref","is-referenced-by-count":12,"title":["Interactions of some partial agonists with high and low affinity binding sites in \u03b2-adrenoceptors"],"prefix":"10.1139","volume":"65","author":[{"given":"I.","family":"Takayanagi","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"K.","family":"Koike","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"A.","family":"Nakagoshi","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"155","container-title":["Canadian Journal of Physiology and Pharmacology"],"original-title":[],"language":"en","link":[{"URL":"http:\/\/www.nrcresearchpress.com\/doi\/pdf\/10.1139\/y87-004","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2020,1,5]],"date-time":"2020-01-05T10:18:48Z","timestamp":1578219528000},"score":1,"resource":{"primary":{"URL":"http:\/\/www.nrcresearchpress.com\/doi\/10.1139\/y87-004"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[1987,1,1]]},"references-count":0,"journal-issue":{"issue":"1","published-print":{"date-parts":[[1987,1,1]]}},"alternative-id":["10.1139\/y87-004"],"URL":"https:\/\/doi.org\/10.1139\/y87-004","relation":{},"ISSN":["0008-4212","1205-7541"],"issn-type":[{"value":"0008-4212","type":"print"},{"value":"1205-7541","type":"electronic"}],"subject":[],"published":{"date-parts":[[1987,1,1]]}}}