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Endocrinology, Vol 100, 629-634, Copyright © 1977 by Endocrine Society
ARTICLES |
A Mahgoub and H Sheppard
Department of Cell Biology, Roche Research Center, Hoffmann-La Roche, Inc., Nutley, New Jersey 07110.
Several hydroxy vitamin D3 (OH-D3) derivatives were tested for biological activity by measuring 45Ca release from prelabeled rat fetal bones, in vitro. In a 72 h continuous culture, 1 alpha,25-(OH)2-D3 produced a significant effect at 10 pg/ml. A similar effect was produced by 50 ng/ml of either 25-OH-D3 or 5,6-trans-25-OH-D3, and by 500 pg of 3 deoxy-1 alpha,25-(OH)2-D3. 24R,25-(OH)2-D3 was more active than 24S,25-(OH)2-D3, and the R isomer had activity that more closely resembled the biosynthetic compound. 3-deoxy-1 alpha-OH-D3 was inactive at a concentration of up to 1 microgram/ml. Using a 24 h preincubation period with no added vitamin D3 derivative, a steep dose-response curve could be obtained with 1 alpha,25-(OH)2-D3 over a range of 2-10 pg/ml during a subsequent 96 h incubation period, and 1 alpha,25-(OH)2-D3 was found to have about 5000 times the activity of 25-OH-D3.
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H. Gelbard, P. Stern, and D. U'Prichard 1 alpha, 25-Dihydroxyvitamin D3 nuclear receptors in pituitary Science, September 12, 1980; 209(4462): 1247 - 1249. [Abstract] [PDF] |
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