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Propranolol is the most investigated \u03b2\u2010blocker for cancer; although as many different off\u2010patent \u03b2\u2010blockers exist, there is little commercial incentive to drive comparative clinical trials. To minimize any chance of endogenous \u03b2\u2010agonist driven cancer growth or metastasis, theoretically, the \u201cideal\u201d anti\u2010cancer \u03b2\u2010blocker would have high affinity, no partial agonism, and long duration of action at \u03b22\u2010adrenoceptors (and for some cancers, additionally at \u03b21 or \u03b23\u2010AR). Using CHO cells stably expressing the wildtype and polymorphic variants of the human \u03b21 and \u03b21\u2010adrenoceptors, this study assessed 35 \u03b2\u2010blockers for the affinity and duration of binding (using\n                    <jats:sup>3<\/jats:sup>\n                    H\u2010CGP12177 whole cell binding) and intrinsic efficacy (CRE\u2010gene transcription). Despite high affinity, some \u03b2\u2010blockers had a short binding duration (e.g., alprenolol, bupranolol, levobunolol, nadolol and oxprenolol). Other compounds had substantial partial agonism (e.g., cyanopindolol, bucindolol, pindolol, pronethalol and xamoterol) and other compounds had a biphasic washout (e.g., bucindolol, timolol, carpindolol, and CGP12177) for reasons unknown. Considering all 3 factors, carazolol and ICI118551 may be more \u201cideal\u201d than propranolol; however, carvedilol, with higher affinity and substantially longer duration of \u03b22 (and \u03b21) receptor binding than propranolol whilst maintaining low partial agonism, may be the most theoretically optimal. Furthermore, it is already widely used in cardiovascular medicine as an off\u2010patent tablet. Thus, carvedilol may have more optimal molecular pharmacological characteristics for an \u201canti\u2010cancer\u201d \u03b2\u2010blocker than propranolol and could enter prospective comparative clinical trials without needing any further clinical workup.\n                  <\/jats:p>","DOI":"10.1002\/prp2.70214","type":"journal-article","created":{"date-parts":[[2026,1,4]],"date-time":"2026-01-04T05:19:48Z","timestamp":1767503988000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":2,"title":["Comparing the Molecular Pharmacological Properties of Existing \u03b2\u2010Blockers to Determine the Theoretically Most \u201cIdeal\u201d Anti\u2010Cancer \u03b2\u2010Blocker"],"prefix":"10.1002","volume":"14","author":[{"given":"Jillian G.","family":"Baker","sequence":"first","affiliation":[{"name":"Cell Signalling, COMPARE, School of Life Sciences, C Floor Medical School Queen's Medical Centre, University of Nottingham  Nottingham 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