Biological activity of fluorine-substituted 1,25-dihydroxyvitamin D3 in rats, in chicken and in Japanese quails.
The biological activity of two fluorinated analogs of 1,25(OH)2D3 was compared with 1,25(OH)2D3 in various vitamin D assays. The effect of 24,24-F2-1,25(OH)2D3 on plasma calcium, bone weight and duodenal calcium binding protein in chicken, on calcium excretion via egg shell in Japanese quails and on mobilization of calcium from the bone in rats was twice as high as the effect of the most potent naturally occurring vitamin D3 metabolite 1,25(OH)2D3. In contrast, 24R-F-1,25(OH)2D3 has less than 50% of the potency of 1,25(OH)2D3. Due to the wider therapeutic dosage range, this compound might be of clinical value.
D000818:Animals; D001835:Body Weight / Q000187:drug effects; D001842:Bone and Bones / Q000187:drug effects* / Q000378:metabolism; D002117:Calcitriol / Q000031:analogs & derivatives* / Q000627:therapeutic use; D002118:Calcium / Q000097:blood / Q000378:metabolism*; D002645:Chickens; D003370:Coturnix; D004305:Dose-Response Relationship, Drug; D004386:Duodenum / Q000378:metabolism; D004528:Egg Shell; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D064030:S100 Calcium Binding Protein G / Q000096:biosynthesis; D014808:Vitamin D Deficiency / Q000188:drug therapy*
D064030:S100 Calcium Binding Protein G; C023370:24,24-difluoro-1,25-dihydroxyvitamin D3; C048149:24-fluoro-1,25-dihydroxycholecalciferol; D002117:Calcitriol; D002118:Calcium