Mechanism by Which 3-Enol Etherification Enhances the Oral Activity of Methyltestosterone in Rats

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Abstract
The mechanism by which 3- enol etherification enhances the oral activity of methyltestosterone has been investigated in castrated male albino rats. It has been shown that the greater intensity and more prolonged activity exhibited by methyltestosterone-3-cyclopentyl enol ether (MTCPE), as compared with methyltestosterone (MT), is not dependent on a decreased rate of intestinal absorption, since both steroids were absorbed at approximately the same rate. Storage in and release from body fat is responsible for such a phenomenon. The observation that MTCPE is stored in body fat is against the theory of its transformation to MT in the gut. In fact, if transformation had occurred either in the intestine or in the liver, no storage in body fat would have been observed. Storage in and release from body fat may also have a bearing on the difference in parallelism between the dose-response curves following the daily oral administration of MTCPE and MT observed in previous experiments (6). (Endocrinology74: 79, 1964)