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Affinity of trazodone for human penile α 1 ‐ andα 2 ‐adrenoceptors
Author(s) -
Krege S.,
Goepel M.,
Sperling H.,
Michel M.C.
Publication year - 2000
Publication title -
bju international
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.773
H-Index - 148
eISSN - 1464-410X
pISSN - 1464-4096
DOI - 10.1046/j.1464-410x.2000.00601.x
Subject(s) - trazodone , erectile dysfunction , radioligand , alpha (finance) , adrenergic receptor , endocrinology , receptor , medicine , antidepressant , pharmacology , chemistry , biology , construct validity , nursing , hippocampus , patient satisfaction
Objective To determine the affinities of human penile α‐adrenoceptors and cloned human α‐adrenoceptor subtypes for trazodone, an antidepressant with reported beneficial effects in erectile dysfunction. Materials and methods Competition radioligand binding studies were performed with trazodone in human penile tissue and in cell lines stably expressing all cloned human α‐adrenoceptor subtypes. Results Trazodone had higher affinity for human α 1 ‐adrenoceptors (10–130 nmol/L) than for α 2 ‐adrenoceptors (300–700 nmol/L), but did not discriminate between subtypes of human α 1 ‐ or α 2 ‐adrenoceptors. Conclusion Trazodone has high and moderate affinity for human α 1 ‐ and α 2 ‐adrenoceptors, respectively; this might contribute to its reported beneficial effects in erectile dysfunction.