Synthesis of (6-3H)-1alpha-hydroxyvitamin D3 and its metabolism in vivo to (3H)-1alpha,25-dihydroxyvitamin D3
Synthesis of (6-3H)-1alpha-hydroxyvitamin D3 and its metabolism in vivo to (3H)-1alpha,25-dihydroxyvitamin D3
复制标题
(6-3H)-1α-羟基维生素 D3 的合成及其体内代谢为 (3H)-1α,25-二羟基维生素 D3
作者：
M. Holick;S. A. Holick;T. Tavela;B. Gallagher;H. Schnoes;H. DeLuca
[6- 3 H]-1 α-羟基维生素D_3经化学合成，证明其具有完全的生物活性和放化纯度。通过使用该制剂，已经可以在体内证明在大鼠中[6- 3 H]-1 α-羟基维生素D3转化为天然激素[6- 3 H]-1 α，25-二羟基维生素D3。事实上，在每天给予32皮摩尔[6- 3 H]-1 α-羟基维生素D3 6天的大鼠的肠道和骨骼中，超过80%的脂溶性放射性以[6- 3 H]-1 α，25-二羟基维生素D3的形式存在，这一发现表明1 α-羟基维生素D3的生物学功效大部分是由于其转化为1 α，25-二羟基维生素D3。
[6-3H]-1alpha-Hydroxyvitamin D3 was chemically synthesized and its full biological activity and radiochemical purity were demonstrated. With the use of this preparation it has been possible to demonstrate in vivo that in rats the [6-3H]-1Alpha-hydroxyvitamin D3 is converted to [6-3H]-1alpha,25-dihydroxyvitamin D3, the natural hormone. In fact, in the intestine and bone of rats given 32 picomoles of [6-3H]-1alpha-hydroxyvitamin D3 each day for 6 days, more than 80 percent of the lipid-soluble radioactivity exists as [6-3H]-1alpha,25-dihydroxyvitamin D3, a finding that suggests that much of the biological effectiveness of 1alpha-hydroxyvitamin D3 is due to its conversion to 1alpha,25-dihydroxyvitamin D3.