Regulatory activities of 2 beta-(3-hydroxypropoxy)-1 alpha, 25-dihydroxyvitamin D3, a novel synthetic vitamin D3 derivative, on calcium metabolism.
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.
Okano
T
T
Department of Hygienic Sciences, Kobe Women's College of Pharmacy, Japan.
Tsugawa
N
N
Masuda
S
S
Takeuchi
A
A
Kobayashi
T
T
Takita
Y
Y
Nishii
Y
Y
D000818:Animals; D001842:Bone and Bones / Q000187:drug effects / Q000503:physiopathology; D002117:Calcitriol / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology*; D002118:Calcium / Q000378:metabolism*; D004195:Disease Models, Animal; D005260:Female; D066298:In Vitro Techniques; D007408:Intestinal Absorption / Q000187:drug effects*; D007700:Kinetics; D008297:Male; D008903:Minerals / Q000032:analysis; D010024:Osteoporosis / Q000503:physiopathology; D010052:Ovariectomy; D051381:Rats; D011916:Rats, Inbred F344; D011919:Rats, Inbred Strains; D018167:Receptors, Calcitriol; D011987:Receptors, Steroid / Q000378:metabolism; D012016:Reference Values; D013329:Structure-Activity Relationship; D014807:Vitamin D / Q000031:analogs & derivatives; D014808:Vitamin D Deficiency / Q000378:metabolism*; D014809:Vitamin D-Binding Protein / Q000378:metabolism
D008903:Minerals; D018167:Receptors, Calcitriol; D011987:Receptors, Steroid; D014809:Vitamin D-Binding Protein; D014807:Vitamin D; D002117:Calcitriol; C547512:eldecalcitol; D002118:Calcium