Abstract
The ability of four vitamin D analogs to inhibit the liver microsomal vitamin D-25-hydroxylase was determined. 19-Hydroxy-10(S), 19-dihydrovitamin D 3,25-fluorovitamin D 3, 3β-hydroxy-9, 10-seco-5, 7, 10(19)-choletrien-24-oic acid dimethylamide and 25-aza-vitamin D 3 were competitive inhibitors with apparent K I values of 44, 137, and 870 n m, and 6.4 μ m, respectively. The values for the 19-hydroxy-10(S), 19-dihydrovitamin D 3, 25-fluorovitamin D 3, and 25-azavitamin D 3 correspond well to other literature reports with respect to their relative in vivo inhibitory properties. 24-Oxovitamin D 3 oxime also proved to be a potent inhibitor but a detailed analysis was prohibited by the lack of material. The 3β-hydroxy-9, 10-seco-5, 7, 10(19)-choletrien-24-oic acid dimethylamide was also tested in vivo but had no antagonistic activity when provided at a 2000-fold excess over vitamin D 3.
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