{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2023,10,9]],"date-time":"2023-10-09T06:11:37Z","timestamp":1696831897830},"reference-count":30,"publisher":"Wiley","issue":"4","license":[{"start":{"date-parts":[[2012,1,11]],"date-time":"2012-01-11T00:00:00Z","timestamp":1326240000000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Journal Cellular Physiology"],"published-print":{"date-parts":[[2012,4]]},"abstract":"<jats:title>Abstract<\/jats:title><jats:p>Positron emission tomography (PET) is an imaging technique that provides direct measurements of receptor binding in neurons. The present study was performed to find reasons for the common observation of rapid metabolism of receptor radioligands during time of a brain PET scan. To this aim, the 1\u2010h phase during which imaging\u2010data are acquired was evaluated by using a pharmacokinetic approach. The values of half\u2010lives, volumes of distribution, and dilution calculated for a set of metabolite corrected plasma curves of D2\u2010receptor radioligand [<jats:sup>11<\/jats:sup>C]raclopride (PETc) during 50\u2009min after radioligand injection in tracer dose were compared with the reference values obtained from a set of plasma curves (REFc) during 30\u2009h after i.v. infusion of unlabelled raclopride in pharmacological doses. We found that the half\u2010life of PETc correspond to the distribution half\u2010life of REFc. Accordingly, the distribution volume during the terminal phase of PETc (13.6\u2009\u00b1\u200910.8\u2009L) was significantly lower than that during the terminal phase (82.2\u2009\u00b1\u200930.5\u2009L) and at steady state (59.4\u2009\u00b1\u200920\u2009L) for REFc, and the dilution of raclopride in body for PETc at 50\u2009min was 38\u2009L, whereas it was 1015\u2009L for REFc at 30\u2009h. The [<jats:sup>11<\/jats:sup>C]raclopride in plasma at 50\u2009min was higher (10% of dose) than the value for unlabelled raclopride at 30\u2009h (4%). We concluded that the kinetic behavior of the radiolabelled drug [<jats:sup>11<\/jats:sup>C]raclopride during the 1\u2009h time of a PET corresponds to the distribution phase. The high percentage of [<jats:sup>11<\/jats:sup>C]raclopride in plasma during this phase is a likely reason for the observed rapid radioligand metabolism. J. Cell. Physiol. 227: 1663\u20131669, 2012. \u00a9 2011 Wiley Periodicals, Inc.<\/jats:p>","DOI":"10.1002\/jcp.22890","type":"journal-article","created":{"date-parts":[[2011,6,15]],"date-time":"2011-06-15T14:56:51Z","timestamp":1308149811000},"page":"1663-1669","source":"Crossref","is-referenced-by-count":0,"title":["Pharmacokinetic analysis of plasma curves obtained after i.v. injection of the PET radioligand [11C] raclopride provides a likely explanation for rapid radioligand metabolism"],"prefix":"10.1002","volume":"227","author":[{"given":"Stelvio","family":"Sestini","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Christer","family":"Halldin","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Luigi","family":"Mansi","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Antonio","family":"Castagnoli","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Lars","family":"Farde","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2012,1,11]]},"reference":[{"key":"e_1_2_6_2_1","doi-asserted-by":"publisher","DOI":"10.1109\/TAC.1974.1100705"},{"key":"e_1_2_6_3_1","first-page":"15N","article-title":"Final PET CGMP regulation","volume":"51","author":"Breslow K","year":"2010","journal-title":"J Nucl Med"},{"key":"e_1_2_6_4_1","doi-asserted-by":"publisher","DOI":"10.1002\/bdd.656"},{"key":"e_1_2_6_5_1","doi-asserted-by":"publisher","DOI":"10.1002\/(SICI)1098-2396(199911)34:2<124::AID-SYN5>3.0.CO;2-O"},{"key":"e_1_2_6_6_1","first-page":"79","article-title":"Radioligand studies in brain: Kinetic analysis of PET data","volume":"5","author":"Cunningham VJ","year":"1995","journal-title":"Med Chem Res"},{"key":"e_1_2_6_7_1","first-page":"R651","article-title":"Multiexponential, multicompartmental, and noncompartmental modeling. 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