Abstract
17α-Ethynylestradiol-17β (β- D -glucuronide) [EE 217β(βG)], a metabolite of 17α-ethynylestradiol (EE 2) identified in urine of women taking EE 2 in oral contraceptives, and its synthetic anomer, 17α-ethynylestradiol-17β(α- D -glucuronide), [EE 217β(αG)], were administered intravenously to female rats in order to determine their effects on bile flow. Both agents induced an immediate, profound and dose-dependent decrease in bile flow which returned to control levels within 1–8 hr. The logarithm of the dose vs the cholestatic response curves for the two anomers were not parallel. EE 217β(αG) was significantly more potent than EE 217β(βG) such that the doses inhibiting bile flow by 50% were 1.25 and 11 μmol/kg for the α- and β-anomer respectively.
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