In:
Journal of Endocrinology, Bioscientifica, Vol. 110, No. 3 ( 1986-09), p. 489-497
Abstract:
In an attempt to define pharmacological probes with which to test the role of catechol oestrogen formation in the central nervous system, five oestrogens (oestradiol-17β, oestradiol-17α, 4-fluoro-oestradiol, 2-fluoro-oestradiol and moxestrol (11β-methoxy-17α-ethynyloestradiol) were studied for binding to oestrogen receptors and conversion to catechol metabolites. Binding to cytosol oestrogen receptors was measured in the hypothalamus–preoptic area–amygdala (HPA), pituitary gland and uterus of ovariectomized rats. Conversion to catechol oestrogens was tested in microsomes from the HPA, pituitary gland and liver, using a catechol- O -methyltransferase-coupled radioenzymatic assay. Oestradiol-17α was the only weak oestrogen receptor ligand. Binding affinities of the other compounds tested were much higher and comparable to those of oestradiol-17β. In contrast, oestradiol-17α was rapidly converted to catechol metabolites, while moxestrol was a relatively poor substrate for catechol oestrogen formation. 4-Fluoro-oestradiol could be 2-hydroxylated but not 4-hydroxylated. 2-Fluoro-oestradiol exhibited impaired 2-hydroxylation but normal 4-hydroxylation. J. Endocr. (1986) 110, 489–497
Type of Medium:
Online Resource
ISSN:
0022-0795
,
1479-6805
DOI:
10.1677/joe.0.1100489
Language:
Unknown
Publisher:
Bioscientifica
Publication Date:
1986
detail.hit.zdb_id:
1474892-7