Abstract
The metabolism of 3H labeled ST-630 [(+)-(5Z, 7E)-26, 26, 26, 27, 27, 27-hexafluoro-9, 10-secocholesta-5, 7, 10(19)-triene-1α, 3β, 25-triol], a new fluorine-substitated analog of 1α, 25-dihydroxyvitamin D3, was studied after single administration in rats. 1. After oral administration to rats, the ST-630 was detected as the main component and a small amount of ST-232, C23-hydroxylated bioactive metabolite of ST-630, was also detected in serum. 2. After oral administration to rats, ST-630, ST-232 and calcitroic acid were exc reted into the bile asglucuronides or other conjugates. 3. In the small intes tine and kidney, the target organs of 1α, 25-dihydroxyvitamin D3, the major components of radioactivity were ST-630 and ST-232. At 24 hr after oral administration, ST-232 was detected predominantly in these tissues. 4. The metabolic pat hway of ST-630 in rats was partially similar to that of 1α, 25-dihydroxyvitamin D3, which is finally metabolized to calcitroic acid and glucuronides. However, ST-630 was mainly metabolized to the bioactive metabolite, ST-232, which was retained in target tissues, causing greater potency of ST-630 than 1α, 25-dihydroxyvitamin D3.
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