Effect on Carbon Lengthening at the Side Chain Terminal of 1α, 25-Dihydroxyvitamin D_3 for Calcium Regulating Activity

概要

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A series of analogs of 1α, 25-dihydroxyvitamin D_3 [1,25-(OH)_2D_3 (1)] with alkyl substitutions in 26- and 27- positions have been tested for their activity 1) in competing with 1,25-(OH)_2D_3 for binding to chick intestinal cytosol receptor, 2) in ability for formation of multinucleated cells (MNC) with various osteoclastic cell characteristics from blast cells, and 3) in stimulating bone calcium mobilization in vitamin D-deficient rats. The relative potencies of 1,25-(OH)_2D_3,1α, 25-dihydroxy-26,27-dimethylvitamin D_3 (2), 1α, 25-dihydroxy-26,27-diethylvitamin D_3 (3), and 1α, 25-dihydroxy-26,27-dipropylvitamin D_3 (4) in competing for intestinal cytosolic binding were 1 : 1.1 : 0.25 : 0.05. The similar order of the abilities on formation of the multinucleated cells in the same series was observed. In a bone calcium mobilization test with vitamin D-deficient rats, 1α, 25-dihydroxy-26,27-dimethylvitamin D_3 showed slightly less activity than 1,25-(OH)_2D_3 at 12h after administration, but long lasting activity was observed during time course experiments. 1α, 25-Dihydroxy-26,27-diethylvitamin D_3,and 1α, 25-dihydroxy-26,27-dipropylvitamin D_3 were found to be much less active than 1,25(OH)_2D_3 in a bone calcium mobilization test.
社団法人日本薬学会の論文
1990-05-25