Work

Competition of the Histamine H2Antagonist Cimetidine for Androgen Binding Sites in Man

Year: 1980
Type: article
Abstract: Gynecomastia and impotence have been described as side‐effects of cimetidine therapy. It has previously been shown that cimetidine possesses antiandrogenic properties and competes for dihydrotestosterone (DHT) binding to the cytosol and nuclear fractions of the rat prostate. Because this interaction may be relevant to the clinical findings in man, the authors analyzed the effects of cimetidine on androgen binding to the human prostate, testis, and serum. Cimetidine competed for DHT binding sites in the human prostate with a displacement curve parallel to that of nonlabeled DHT, whereas no binding to the testis or serum was apparent. Neither histamine nor the H1antagonist diphenhydramine was capable of inhibiting androgen binding to the human prostate. Thus, androgen antagonism may be the mechanism of the endocrine side‐effects of cimetidine in man.
Language: English
Field: Medicine
Open Access status: bronze
OpenAlex ID: W1541588807
FWCI: 0.622
Cites: 28
Cited by: 9
Related to: 10