Metabolites In Healthy Subjects Research Articles

Metabolism of 1-dehydroandrostanes in man: II—Metabolism of 5β-androst-1-enes

In order to better understand the results of a previous study on the metabolism of 3-keto-1,4-androstadienes, the excretion of urinary metabolites in healthy subjects after oral administration of 5β-androst-1-ene-3,17-dione (I), 17β-hydroxy-5β-androst-1-en-3-one (II), 3α-hydroxy-5β-androst-1-ene-17-one (III) and 5β-androst-1-ene-3α,17β-diol(IV) have been investigated. The main features of the metabolism of these compounds were the large survival of C 1-C 2 double bond in the metabolites, reduction to etiocholanolone being relatively important only after IV, and the significant excretion of 17β-hydroxysteroids, chiefly after I and II.

Metabolism of 1-dehydroand rostanes in man: I. Metabolism of 17β-hydroxyandrosta-1, 4-dien-3-one, 17β-cyclopent-1'-enyloxyandrosta-1, 4-dien-3-one (quinbolone) and androsta-1, 4-diene-3, 17-dione

The excretion of urinary metabolites in healthy subjects after oral administration of 17β-hydroxyandrosta-1,4-dien-3-one (II) and its 17-cyclopentenyl ether (quinbolone, I), an orally active anabolic agent, has been comparatively investigated. The excretion pattern proved to be very similar for the two compounds, thus confirming the lability in vivo of the ether linkage of I to give II. A similar catabolite excretion has been observed also after ingestion of androsta-1, 4-diene-3, 17-dione (III). The Δ 1-double bond has been found to survive metabolism to a great extent. The Δ 1,4-dien-3-one group was still unchanged in about 40% of the metabolites excreted and most of the remaining ones were Δ 1-3-keto- or Δ 1-3a-hydroxy-5β-compounds. Moreover, a remarkable amount of 6β-hydroxy-Δ 1,4-3-ketones has been identified. The most interesting feature of the metabolism of I, II and III was the high excretion of 17β-hydroxysteroids.