Metabolism of 1,1-dichloro-cis-diphenylcyclopropane by rat liver microsomes.
The metabolic fate of the anti-estrogen 1,1-dichloro-cis-diphenylcyclopropane (Analog II), was studied in vitro with phenobarbital-induced rat liver microsomal fractions. The presence of five metabolites was directly or indirectly established. Biotransformation products were isolated by TLC and HPLC techniques and, when possible, the structures were confirmed through comparison with synthetic samples. The presence of an allyl chloride, highly reactive, metabolic intermediate was stated.
Caputo
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O
Istituto di Chimica Farmaceutica Applicata, Università di Torino, Italia.
Grosa
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G
Ceruti
M
M
Rocco
F
F
Biglino
G
G
D000818:Animals; D001711:Biotransformation; D002851:Chromatography, High Pressure Liquid; D002855:Chromatography, Thin Layer; D004965:Estrogen Antagonists / Q000737:chemistry / Q000378:metabolism*; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D008862:Microsomes, Liver / Q000378:metabolism*; D051381:Rats; D011919:Rats, Inbred Strains; D011960:Receptors, Estrogen / Q000378:metabolism; D013629:Tamoxifen / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism
D004965:Estrogen Antagonists; D011960:Receptors, Estrogen; D013629:Tamoxifen; C035174:tamoxifen analog II