Abstract
Several histamine H 2 receptor antagonists have been tested for antiandrogenic activity by determining their effects on accessory sex organ weights in castrate testosterone propionate (TP) treated rats and on [ 3H]dihydrotestosterone (DHT) binding to the androgen receptor of the rat ventral prostate in vitro. When given in high doses cimetidine and metiamide possessed antiandrogenic activity whereas the other H 2 receptor antagonists SK&F 92456, SK&F 92994, SK&F 92629 and SK&F 93479 did not. Cimetidine, metiamide and SK&F 92456 inhibited [ 3H]DHT binding to rat ventral prostate androgen receptor in vitro whereas SK&F 92629 and SK&F 93479 did not. SK&F 92994 affects DHT binding only slightly. Of the compounds that are similar to cimetidine in their potency as H 2 receptor antagonists only metiamide was antiandrogenic. However SK&F 92994 and SK&F 93479 are not antiandrogenic despite being more potent than cunetidine as H 2 antagonists. It is concluded that the antiandrogenicity of cimetidine and metiamide was not related to their activity as histamine H 2 receptor antagonists.
Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
