WS-9659 A and B, novel testosterone 5 alpha-reductase inhibitors isolated from a Streptomyces. III. Biological characteristics and pharmacological characteristics.
WS-9659 A, a novel phenazine, produced by a Streptomyces sp., had testosterone 5 alpha-reductase inhibition activity on rat, dog and human prostates. However, WS-9659 A did not show any inhibitory activities for aldose reductase on rabbit lenses and lactate dehydrogenase on pig hearts. WS-9659 A was a competitive inhibitor against testosterone 5 alpha-reductase on rat prostates by use of testosterone as a substrate. Radio receptor binding assay of androgen receptor of rat prostates revealed that WS-9659 A had no affinity for this receptor. WS-9659 A was tested subcutaneously in immature castrated rats to confirm its effect on the growth of the ventral prostates induced by testosterone propionate.
Nakayama
O
O
Exploratory Research Laboratory, Fujisawa Pharmaceutical Co., Ltd., Ibaraki, Japan.
Arakawa
H
H
Yagi
M
M
Tanaka
M
M
Kiyoto
S
S
Okuhara
M
M
Kohsaka
M
M
D058891:5-alpha Reductase Inhibitors; D000449:Aldehyde Reductase / Q000037:antagonists & inhibitors; D000818:Animals; D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D004285:Dogs; D006801:Humans; D066298:In Vitro Techniques; D007770:L-Lactate Dehydrogenase / Q000037:antagonists & inhibitors; D008297:Male; D009919:Orchiectomy; D009929:Organ Size / Q000187:drug effects; D010619:Phenazines / Q000494:pharmacology*; D011467:Prostate / Q000187:drug effects / Q000201:enzymology; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains; D011944:Receptors, Androgen / Q000378:metabolism; D013552:Swine
D058891:5-alpha Reductase Inhibitors; D000900:Anti-Bacterial Agents; D010619:Phenazines; D011944:Receptors, Androgen; C060460:lavanducyanin; C060647:WS 9659 B; D000449:Aldehyde Reductase; D007770:L-Lactate Dehydrogenase