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They play an important role in drug disposition and drug-drug interactions (DDIs) and have been associated with various diseases. PET with 6-bromo-7-[<jats:sup>11<\/jats:sup>C]methylpurine ([<jats:sup>11<\/jats:sup>C]BMP) has been used to assess MRP1 function in the brain and lungs of mice. [<jats:sup>11<\/jats:sup>C]BMP crosses cellular membranes by passive diffusion followed by intracellular conjugation with glutathione and MRP1-mediated efflux of the radiolabelled glutathione-conjugate. In this study, we assessed the effect of the prototypical organic anion transporter inhibitor probenecid on the whole-body disposition of [<jats:sup>11<\/jats:sup>C]BMP to examine its suitability for measuring the function of MRP1 and possibly other MRP subtypes across multiple tissues.<\/jats:p>\n          <\/jats:sec>\n          <jats:sec>\n            <jats:title>Methods<\/jats:title>\n            <jats:p>Seven healthy volunteers (3 women, 4 men) underwent two dynamic whole-body PET scans on a long axial field-of-view (LAFOV) PET\/CT system after intravenous injection of [<jats:sup>11<\/jats:sup>C]BMP, without and with pre-treatment with a single oral dose of probenecid. Volumes of interest were outlined for several MRP-expressing tissues (cerebral cortex, cerebellum, choroid plexus, retina, lungs, myocardium, skeletal muscle, kidneys, and liver). Tissue time-activity curves were corrected for the contribution of vascular radioactivity and the elimination rate constant (<jats:italic>k<\/jats:italic>\n              <jats:sub>E<\/jats:sub>, h<jats:sup>\u2212\u20091<\/jats:sup>) was calculated as a parameter for tissue MRP function.<\/jats:p>\n          <\/jats:sec>\n          <jats:sec>\n            <jats:title>Results<\/jats:title>\n            <jats:p>Radioactivity was primarily excreted into the urinary bladder and urinary clearance was significantly decreased after probenecid administration (\u2212\u200950\u2009\u00b1\u200916%). Following probenecid administration, <jats:italic>k<\/jats:italic>\n              <jats:sub>E<\/jats:sub> was significantly decreased in the kidneys (\u2212\u200943\u2009\u00b1\u200920%), liver (\u2212\u200918\u2009\u00b1\u200915%), myocardium (\u2212\u200916\u2009\u00b1\u200912%), skeletal muscle (\u2212\u200951\u2009\u00b1\u200934%), and retina (\u2212\u200957\u2009\u00b1\u200929%, non-blood-corrected).<\/jats:p>\n          <\/jats:sec>\n          <jats:sec>\n            <jats:title>Conclusion<\/jats:title>\n            <jats:p>Our study highlights the great potential of LAFOV PET\/CT to assess drug disposition and transporter-mediated DDIs in humans at a whole-body, multi-tissue level. Due to the slow elimination of [<jats:sup>11<\/jats:sup>C]BMP-derived radioactivity from the human brain, [<jats:sup>11<\/jats:sup>C]BMP appears unsuitable to measure cerebral MRP1 function in humans, but it may be used to assess the function of MRP1 and possibly other MRP subtypes in various peripheral tissues.<\/jats:p>\n          <\/jats:sec>\n          <jats:sec>\n            <jats:title>Trial registration<\/jats:title>\n            <jats:p>EudraCT 2021-006348-29. Registered 15 December 2021.<\/jats:p>\n          <\/jats:sec>","DOI":"10.1007\/s00259-025-07121-5","type":"journal-article","created":{"date-parts":[[2025,2,8]],"date-time":"2025-02-08T03:12:23Z","timestamp":1738984343000},"page":"2477-2490","update-policy":"https:\/\/doi.org\/10.1007\/springer_crossmark_policy","source":"Crossref","is-referenced-by-count":2,"title":["Effect of probenecid on the whole-body disposition of 6-bromo-7-[11C]methylpurine in humans assessed with long axial field-of-view PET\/CT"],"prefix":"10.1007","volume":"52","author":[{"given":"Matthias","family":"Jackwerth","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Severin","family":"Mairinger","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ivo","family":"Rausch","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Maria","family":"Weber","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Anselm","family":"Jorda","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Lukas","family":"Nics","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Werner","family":"Langsteger","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Markus","family":"Zeitlinger","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Marcus","family":"Hacker","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Oliver","family":"Langer","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"297","published-online":{"date-parts":[[2025,2,8]]},"reference":[{"key":"7121_CR1","doi-asserted-by":"publisher","first-page":"67","DOI":"10.1146\/annurev.cb.08.110192.000435","volume":"8","author":"CF Higgins","year":"1992","unstructured":"Higgins CF. 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