Chemical and Pharmaceutical Bulletin p. 215 - 219 (2000)
Update date:2022-08-03
Topics:
Kawase, Akira
Ichikawa, Fumihiko
Koike, Nobuo
Kamachi, Shinichi
Stumpf, Walter E.
Nishii, Yasuho
Kubodera, Noboru
A novel synthesis of a radioactive compound of 1α-hydroxyvitamin D3 (1αOHD3) (1) and its pharmacokinetics are described. Radioactive 1αOHD3 tritiated at 22 and 23 positions ([22,23-3H4]1αOHD3) (5) was prepared via key reactions of the reduction of acetylenic side chain in the ketone (12) with tritium gas in the presence of palladium-charcoal and the subsequent Wittig reaction with the A-ring synthon (16). [22,23-3H4]1αOHD3 (5) showed high specific radioactivity (111.5 Ci/mmol) and was used successfully in pharmacokinetics studies with rats. In the pharmacokinetics studies, the plasma concentration level of the active form of vitamin D3, 1α,25- dihydroxyvitamin D3 [1α,25(OH)2D3], after oral or intravenous administration of [22,23-3H4]1αOHD3 (5), showed longer half-life, lower maximum concentration, and lower area under the curve than those after treatment of 1α,25(OH)2D3 tritiated at 26 and 27 positions (4). These results might suggest a beneficial therapeutic utility of 1αOHD1 (1) over the treatment of 1α,25(OH)2D3 (2).
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(2000)