Regulatory activities of 2 beta-(3-hydroxypropoxy)-1 alpha, 25-dihydroxyvitamin D3, a novel synthetic vitamin D3 derivative, on calcium metabolism

Biochem Biophys Res Commun. 1989 Sep 29;163(3):1444-9. doi: 10.1016/0006-291x(89)91140-6.

Abstract

Regulatory activities of 2 beta-(3-hydroxypropoxy)-1 alpha, 25-dihydroxyvitamin D3 [ED-71], a novel synthetic vitamin D3 derivative, on calcium metabolism were investigated. The compound behaved similar to 1 alpha, 25-dihydroxyvitamin D3 [1,25(OH)2D3] in the ex vivo intestinal calcium transport using rat everted gut sac and the in vivo bone mobilization using vitamin D-deficient rats. By means of Raisz's assay method, 45Ca releasing activity of ED-71 was not greater than that of 1,25(OH)2D3. The time course curve of ED-71 in plasma made a mild round shape compared with that of 1,25(OH)2D3 and the former's plasma concentration remained increased longer than the latter's. The therapeutic effect of ED-71 for the animal models with osteoporosis seemed to be better than that of 1,25(OH)2D3. The results suggest that ED-71 may be a promising drug for therapy of osteoporosis.

MeSH terms

  • Animals
  • Bone and Bones / drug effects
  • Bone and Bones / physiopathology
  • Calcitriol / analogs & derivatives*
  • Calcitriol / metabolism
  • Calcitriol / pharmacology*
  • Calcium / metabolism*
  • Disease Models, Animal
  • Female
  • In Vitro Techniques
  • Intestinal Absorption / drug effects*
  • Kinetics
  • Male
  • Minerals / analysis
  • Osteoporosis / physiopathology
  • Ovariectomy
  • Rats
  • Rats, Inbred F344
  • Rats, Inbred Strains
  • Receptors, Calcitriol
  • Receptors, Steroid / metabolism
  • Reference Values
  • Structure-Activity Relationship
  • Vitamin D / analogs & derivatives
  • Vitamin D Deficiency / metabolism*
  • Vitamin D-Binding Protein / metabolism

Substances

  • Minerals
  • Receptors, Calcitriol
  • Receptors, Steroid
  • Vitamin D-Binding Protein
  • Vitamin D
  • Calcitriol
  • eldecalcitol
  • Calcium