In vitro metabolism of 17α-ethynylsteroids

The rates of metabolism of synthetic gestagens derived from 19-nortestosterone by rabbit liver tissue in vitro were compared. Over a period of 1 h norethisterone was metabolised as rapidly as 19-nortestosterone whereas d-norgestrel and lynestrenol were metabolised at a slightly lower rate. Less than...

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Bibliographic Details
Published inJournal of steroid biochemistry Vol. 10; no. 4; pp. 437 - 442
Main Authors Khan, Firyal S., Potherby, K.
Format Journal Article
LanguageEnglish
Published England Elsevier B.V 01.04.1979
Subjects
Animals
Dihydrotestosterone - metabolism
Female
Liver - metabolism
Male
Norethindrone - metabolism
Norgestrel - metabolism
Organ Specificity
Progesterone Congeners - metabolism
Rabbits
Structure-Activity Relationship
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Summary:The rates of metabolism of synthetic gestagens derived from 19-nortestosterone by rabbit liver tissue in vitro were compared. Over a period of 1 h norethisterone was metabolised as rapidly as 19-nortestosterone whereas d-norgestrel and lynestrenol were metabolised at a slightly lower rate. Less than 5% of l-norgestrel was metabolised. In all cases the reaction product was the tetrahydrosteroid. Lynestrenol was metabolised through norethisterone. Skeletal muscle, lung and small intestine also metabolised norethisterone and d-norgestrel but at a slower rate than liver tissue. Small amounts of norethisterone were metabolised by adipose tissue but heart and spleen were inactive. Lynestrenol and l-norgestrel were not metabolised by any of the extra-hepatic tissues studied.
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ISSN:0022-4731
DOI:10.1016/0022-4731(79)90332-7