Objective To determine the affinities of human penile alpha-adrenoceptors a
nd cloned human alpha-adrenoceptor subtypes for trazodone, an antidepressan
t with reported beneficial effects in erectile dysfunction.
Materials and methods Competition radioligand binding studies were performe
d with trazodone in human penile tissue and in cell lines stably expressing
all cloned human alpha-adrenoceptor subtypes.
Results Trazodone had higher affinity for human alpha(1)-adrenoceptors (10-
130 nmol/L) than for alpha(2)-adrenoceptors (300-700 nmol/L), but did not d
iscriminate between subtypes of human alpha(1)- or alpha(2)-adrenoceptors.
Conclusion Trazodone has high and moderate affinity for human alpha(1)- and
alpha(2)-adrenoceptors, respectively; this might contribute to its reporte
d beneficial effects in erectile dysfunction.