Ent-16α-methylamino-3-methoxy-1,3,5(10)-estratrien-17β-ol hydrochloride, a selective anti-arrhytmic enantiosteroid

Ent-16α-methylamino-3-methoxy-1,3,5(10)-estratrien-17β-ol hydrochloride, a selective anti-arrhytmic enantiosteroid

The title compound and its antipode with natural steroid configuration were synthesized and tested. Both compounds showed equal potency as anti-arrhythmic compounds. An additional effect found for the steroid with natural configuration was its plasma cholesterol lowering activity in the rat. This su...

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Veröffentlicht in:Steroids 1982-12, Vol.40 (6), p.615-623
Hauptverfasser: Boyd, A., Groen, M.B., Hindriksen, B., Marshall, R.J., Sleigh, T., Winslow, E., Zeelen, F.J.
Format: Artikel
Sprache:eng
Schlagworte:
Animals
Anti-Arrhythmia Agents - chemical synthesis
Arrhythmias, Cardiac - drug therapy
Atrial Function
Biological Assay
Cholesterol - blood
Epithelium - drug effects
Estriol - analogs & derivatives
Estriol - chemical synthesis
Estriol - pharmacology
Female
Guinea Pigs
Indicators and Reagents
Magnetic Resonance Spectroscopy
Male
Myocardial Contraction - drug effects
Optical Rotation
Rats
Rats, Inbred Strains
Structure-Activity Relationship
Vagina - drug effects
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Beschreibung
Zusammenfassung:The title compound and its antipode with natural steroid configuration were synthesized and tested. Both compounds showed equal potency as anti-arrhythmic compounds. An additional effect found for the steroid with natural configuration was its plasma cholesterol lowering activity in the rat. This suggests that enantiosteroids may have a more selective action than the steroids with natural configuration
ISSN:0039-128X
1878-5867
DOI:10.1016/0039-128X(82)90002-2