Synthesis and biological activities of 8(14)a-homocalcitriol.
8(14)a-Homocalcitriol was synthesized and tested for its biologic activities. It exhibited a vitamin D agonist activity profile. The compound was bound to the pig intestinal receptor with an affinity slightly less than calcitriol, showed the same potency in inducing HL 60 cell differentiation and inhibition of keratinocyte proliferation as calcitriol, and was found to be approximately 10-fold less potent in inducing hypercalcemia and hypercalciuria after a single injection in normal rats.
Steinmeyer
A
A
Research Laboratories of Schering AG, Berlin, Germany.
Neef
G
G
Kirsch
G
G
Schwarz
K
K
Rach
P
P
Haberey
M
M
Thieroff-Ekerdt
R
R
D000818:Animals; D002117:Calcitriol / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D002118:Calcium / Q000652:urine; D002454:Cell Differentiation / Q000187:drug effects; D002455:Cell Division / Q000187:drug effects; D006801:Humans; D006934:Hypercalcemia / Q000139:chemically induced; D015603:Keratinocytes / Q000187:drug effects; D015394:Molecular Structure; D018167:Receptors, Calcitriol; D011987:Receptors, Steroid / Q000187:drug effects*; D013552:Swine; D014407:Tumor Cells, Cultured; D014809:Vitamin D-Binding Protein / Q000378:metabolism
D018167:Receptors, Calcitriol; D011987:Receptors, Steroid; D014809:Vitamin D-Binding Protein; C078538:8(14)a-homocalcitriol; D002117:Calcitriol; D002118:Calcium