Synthesis and biological activities of 8(14)a-homocalcitriol

A Steinmeyer; G Neef; G Kirsch; K Schwarz; P Rach; M Haberey; R Thieroff-Ekerdt

doi:10.1016/0039-128x(92)90099-u

Synthesis and biological activities of 8(14)a-homocalcitriol

Steroids. 1992 Sep;57(9):447-52. doi: 10.1016/0039-128x(92)90099-u.

Authors

A Steinmeyer¹, G Neef, G Kirsch, K Schwarz, P Rach, M Haberey, R Thieroff-Ekerdt

Affiliation

¹ Research Laboratories of Schering AG, Berlin, Germany.

PMID: 1333655
DOI: 10.1016/0039-128x(92)90099-u

Abstract

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.

MeSH terms

Animals
Calcitriol* / analogs & derivatives*
Calcitriol* / chemical synthesis
Calcitriol* / pharmacology
Calcium / urine
Cell Differentiation / drug effects
Cell Division / drug effects
Humans
Hypercalcemia / chemically induced
Keratinocytes / drug effects
Molecular Structure
Receptors, Calcitriol
Receptors, Steroid / drug effects*
Swine
Tumor Cells, Cultured
Vitamin D-Binding Protein / metabolism

Substances

Receptors, Calcitriol
Receptors, Steroid
Vitamin D-Binding Protein
8(14)a-homocalcitriol
Calcitriol
Calcium