Isolation and Characterization of Urinary Metabolites of 16α-Chloroestrone Methyl Ether in the Rabbit

抄録

The metabolic fate of 16α-chloroestrone methyl ether (I), which is used as a lipidshifting drug, has been investigated in the rabbit. Five principal metabolites were separated from the urine specimen collected after oral administration of I. These metabolites were identified as 16α-chloro-17α-estradiol (II), estrone (III), 16β-chloro-17α-estradiol (IV), 17α-estradiol (V) and 16, 17-epiestriol (VI) by direct comparison with the authentic samples, respectively (see Chart 1). The biochemical significance of in vivo transformation hereby observed has been discussed. The synthesis of the reference compounds for comparison with the metabolites has also been described.