Linked Life Data

7803979

Source:http://linkedlifedata.com/resource/pubmed/id/7803979

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
3
pubmed:dateCreated
1995-1-27
pubmed:abstractText
The estrogen-like effects of norethisterone (NET) seem to be mediated by the interaction of 3 beta 5 alpha- and 3 alpha 5 alpha-tetrahydronorethisterone (3 beta 5 alpha- and 3 alpha 5 alpha-NET, respectively) with the estrogen receptor. Considering that the in vitro uterine contractile response to serotonin (5-HT) is specifically dependent on estrogen, the aim of the present study was to investigate whether NET and its A-ring reduced metabolites administered in vivo to ovariectomized rats induce uterine sensitivity to 5-HT in vitro. The administration of 3 beta NET in vivo, which is the NET metabolite with the highest affinity for the estrogen receptor, induced a maximal contractile response to serotonin similar to that of 17 beta-estradiol treatment. The other metabolites induced less uterine activity. According to the effective dose 50, the order of estrogenic potency was 17 beta-estradiol > 3 beta 5 alpha NET > 3 alpha 5 alpha NET > NET > 5 alpha NET. The estrogenic effect of 3 beta 5 alpha- and 3 alpha 5 alpha NET may be exerted through their interaction with the estrogen receptor, whereas NET and 5 alpha NET, which do not bind to the estrogen receptor and display a minor estrogenic activity, require prior bioconversion to 3 beta 5 alpha NET and perhaps to 3 alpha 5 alpha NET. The A-ring reduced metabolites of NET, mainly the 3 beta 5 alpha NET, may be exerting estrogenic responses and modulating uterine activity when administered in vivo.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
0188-4409
pubmed:author
pubmed:issnType
Print
pubmed:volume
25
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
307-10
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1994
pubmed:articleTitle
Estrogenic actions of norethisterone and its A-ring reduced metabolites. Induction of in vitro uterine sensitivity to serotonin.
pubmed:affiliation
UIM en Farmacología, Hospital de Especialidades, Centro Médico Nacional Siglo XXI, IMSS, México, D.F.
pubmed:publicationType
Journal Article, In Vitro