Detail of "15270-30-1"

Reference

The effect of pregnancy and treatment with 17b-estradiol on the transport of organic anions into isolated rat hepatocytes

The effect of pregnancy and treatment with 17b-estradiol on the transport of organic anions into isolated rat hepatocytes. Brock, William J.; Vore, Mary (Coll. Med., Univ. Kentucky, Lexington, KY 40536, USA). Drug Metab. Dispos., 12(6), 712-16 (English) 1984. CODEN: DMDSAI. ISSN: 0090-9556. DOCUMENT TYPE: Journal CA Section: 2 (Mammalian Hormones) Section cross-reference(s): 13 The uptakes of taurocholic acid (TC) [81-24-3] and of the org. anions estradiol-17b(b-D-glucuronide) (E217G) [1806-98-0], estradiol-3-(b-D-glucuronide) (E23G) [15270-30-1], estriol-16a(b-D-glucuronide) (E316G) [1852-50-2] and morphine glucuronide (MG) [33086-26-9] were evaluated in hepatocytes isolated from nonpregnant female, pregnant (19-21 days of gestation), and E2 [50-28-2]-treated (1 mg/kg/day s.c. for 14 days) rats. Pregnancy decreased the uptake of TC, E217G, E23G, and MG whereas E2 treatment decreased only the uptake of E217G. The Vmax (nmol/min/mg protein) for E217G uptake was decreased from 1.45 in hepatocytes from nonpregnant female rats to 0.70 and 0.64 in cells from pregnant and E2-treated rats, resp. The Vmax for uptake of TC was decreased, but not significantly, from 0.56 in hepatocytes from nonpregnant female rats to 0.34 in cells from pregnant rats.

Characterization of the interaction between estrogen metabolites and taurocholate for uptake into isolated hepatocytes

Characterization of the interaction between estrogen metabolites and taurocholate for uptake into isolated hepatocytes. Lack of correlation between cholestasis and inhibition of taurocholate uptake. Brock, William J.; Durham, Sherrie; Vore, Mary (Coll. Med., Univ. Kentucky, Lexington, KY 40536, USA). J. Steroid Biochem., 20(5), 1181-5 (English) 1984. CODEN: JSTBBK. ISSN: 0022-4731. DOCUMENT TYPE: Journal CA Section: 2 (Mammalian Hormones) Section cross-reference(s): 14 The uptake of 3H-labeled taurocholate (TC) [81-24-3] into isolated rat hepatocytes was examd. in the presence of known cholestatic steroid glucuronides. The cholestatic D-ring glucuronide conjugates of estradiol, estriol, ethynylestradiol, and dihydrotestosterone did not inhibit the uptake of TC suggesting that these org. anions are transported by different carrier systems. Estrone sulfate [481-97-0] inhibited TC uptake 65% but did not decrease bile flow following i.v. administration to the rat (22 mmol/kg), under conditions which estradiol-17b-(b-D-glucuronide) (E217G) [1806-98-0] decreased bile flow 100%. The hepatocyte uptake of [3H]E217G (100 mM) was inhibited by estriol-16a-(b-D-glucuronide) [1852-50-2] (200 mM, 40%) and estradiol-17b-3-(b-D-glucuronide) [15270-30-1] (200 mM, 22%) as well as by the org. anions bromosulfophthalein [71-67-0] (150 mM, 57%), dibromosulfophthalein [17199-35-8] (150 mM, 59%), indocyanine green [3599-32-4] (150 mM, 62%), rose bengal [11121-48-5] (150 mM, 56%), and bilirubin [635-65-4] (50 mM, 40%). Thus, bile acids and steroid glucuronides are transported into the hepatocyte by different carrier systems so that the cholestasis induced by the steroid D-ring glucuronides cannot be explained by an inhibition of bile acid uptake. Furthermore, the hepatocyte uptake of E217G occurs by a carrier system similar to that for the other steroid glucuronides and org. anions.