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This study examined 101 clinical drugs and laboratory compounds to build a comprehensive understanding of \u03b11\u2010adrenoceptor subtype affinity and selectivity. [3H]prazosin whole\u2010cell binding was conducted in CHO cells stably expressing either the full\u2010length human \u03b11A, \u03b11B, or \u03b11D\u2010adrenoceptor. As expected, doxazosin was a high\u2010affinity nonselective \u03b11\u2010antagonist although other compounds (eg, cyclazosin, 3\u2010MPPI, and ARC239) had higher affinities. Several highly \u03b11A\u2010selective antagonists were confirmed (SNAP5089 had over 1700\u2010fold \u03b11A selectivity). Despite all compounds demonstrating \u03b11 affinity, only BMY7378 had \u03b11D selectivity and no \u03b11B\u2010selective compounds were identified. Phenoxybenzamine (used in pheochromocytoma) and dibenamine had two\u2010component\u2010binding inhibition curves at all three receptors. Incubation with sodium thiosulfate abolished the high\u2010affinity component suggesting this part is receptor mediated. Drugs used for hypertension and BPH had very similar \u03b11A\/\u03b11B\/\u03b11D\u2010adrenoceptor pharmacological profiles. Selective serotonin reuptake inhibitors (antidepressants) had poor \u03b11\u2010adrenoceptor affinity. Several tricyclic antidepressants (eg, amitriptyline) and antipsychotics (eg, chlorpromazine and risperidone) had high \u03b11\u2010adrenoceptor affinities, similar to, or higher than, \u03b1 blockers prescribed for hypertension and BPH, whereas others had poor \u03b11 affinity (eg, protriptyline, sulpiride, amisulpiride, and olanzapine). The addition of \u03b1 blockers for the management of hypertension or BPH in people already taking tricyclic antidepressants and certain antipsychotics may not be beneficial. Awareness of the \u03b1\u2010blocking potential of different antipsychotics may affect the choice of drug for those with delirium where additional hypotension (eg, in sepsis) may be detrimental.<\/jats:p>","DOI":"10.1002\/prp2.602","type":"journal-article","created":{"date-parts":[[2020,7,1]],"date-time":"2020-07-01T07:16:37Z","timestamp":1593587797000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":53,"title":["The affinity and selectivity of \u03b1\u2010adrenoceptor antagonists, antidepressants, and antipsychotics for the human \u03b11A, \u03b11B, and \u03b11D\u2010adrenoceptors"],"prefix":"10.1002","volume":"8","author":[{"given":"Richard G. 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