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PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
3
pubmed:dateCreated
1992-12-3
pubmed:abstractText
A series of analogs of 1 alpha,25-dihydroxyvitamin D3[1,25(OH)2D3] with alkyl substitutions in 26- and 27-positions were tested for calcium (Ca) regulating activity. The potencies of dialkyl analogs in stimulating bone resorption in neonatal mouse calvaria cultures were the highest in 1 alpha,25-dihydroxy-26,27-dimethylvitamin D3[1,25(OH)2-(Me)2D3], followed by 1,25(OH)2D3, 1 alpha,25-dihydroxy-26,27-diethylvitamin D3[1,25(OH)2(Et)2D3], and 1 alpha,25-dihydroxy-26,27-dipropylvitamin D3[1,25(OH)2(Pr)2D3] in that order. A similar order of potential regarding formation of osteoclast-like cells in mouse bone marrow cell cultures and on bone Ca mobilization with long-term vitamin D-deficient rats was observed in the same series. The relative potencies of 1,25(OH)2D3, 1,25(OH)2(Me)2D3, 1,25(OH)2(Et)2D3, and 1,25(OH)2(Pr)2D3 in competing with 1,25(OH)2D3 for binding to chick intestinal cytosol receptors were 1:1:0.16:0.036. A similar order of potential in case of intestinal Ca transport in situ was observed in the same series. The potencies of dialkyl analogs in competing with 25-hydroxy-vitamin D3 for binding to rat serum vitamin D binding protein were much lower than that of 1,25(OH)2D3. Effect of 1,25(OH)2(Me)2D3 on osteopenia in rats induced by ovariectomy and right sciatic neurotomy was higher than that of 1,25(OH)2D3. From these results, the lengthening by one carbon at 26- and 27-positions was shown to maintain the Ca regulatory activity of 1,25(OH)2D3.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Sep
pubmed:issn
0171-967X
pubmed:author
pubmed:issnType
Print
pubmed:volume
51
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
218-22
pubmed:dateRevised
2003-11-14
pubmed:meshHeading
pubmed-meshheading:1330237-Animals, pubmed-meshheading:1330237-Biological Transport, pubmed-meshheading:1330237-Bone Diseases, Metabolic, pubmed-meshheading:1330237-Bone Marrow, pubmed-meshheading:1330237-Bone Marrow Cells, pubmed-meshheading:1330237-Bone Resorption, pubmed-meshheading:1330237-Bone and Bones, pubmed-meshheading:1330237-Calcitriol, pubmed-meshheading:1330237-Calcium, pubmed-meshheading:1330237-Cells, Cultured, pubmed-meshheading:1330237-Cytosol, pubmed-meshheading:1330237-Female, pubmed-meshheading:1330237-Intestines, pubmed-meshheading:1330237-Male, pubmed-meshheading:1330237-Mice, pubmed-meshheading:1330237-Osteoclasts, pubmed-meshheading:1330237-Ovariectomy, pubmed-meshheading:1330237-Rats, pubmed-meshheading:1330237-Rats, Wistar, pubmed-meshheading:1330237-Receptors, Cell Surface, pubmed-meshheading:1330237-Sciatic Nerve, pubmed-meshheading:1330237-Vitamin D-Binding Protein
pubmed:year
1992
pubmed:articleTitle
Calcium regulating activity of 26,27-dialkyl analogs of 1 alpha,25-dihydroxyvitamin D3.
pubmed:affiliation
Department of Toxicology, Faculty of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University, Japan.
pubmed:publicationType
Journal Article