Biliary excretion of estradiol-17β-glucuronide in the rat

✍ Scribed by H Takikawa; R Yamazaki; N Sano; M Yamanaka

• Publisher: John Wiley and Sons
• Year: 1996
• Tongue: English
• Weight: 239 KB
• Volume: 23
• Category: Article
• ISSN: 0270-9139
• DOI: 10.1002/hep.510230328

✦ Synopsis

Estradiol-17b-glucuronide (E 2 17G) is a cholestatic dent carriers for ligands are known to exist at the agent and is considered to be related to the pathogenesis canalicular membrane. The first one is a multidrug of intrahepatic cholestasis of pregnancy. In the current resistance gene product, P-glycoprotein (P-GP), study, we examined the mechanism of the biliary excrewhich transports organic cations, such as vinblastine tion of E 2 17G and estradiol metabolites in rats. Biliary (VLB). 6-10 Indeed, the intrahepatic concentration of excretion of tracer doses of [ 3 H]estradiol-17b-glucuro-VLB was reported to increase after its administration nide and [ 14 C]estradiol or [ 3 H]taurocholate and [ 14 C]vinin mdr 1a knockout mice. 11 The second is an ATP-deblastine, a P-glycoprotein (P-GP) substrate, intravependent bile acid carrier, which mainly excretes bile nously administered as a bolus to bile-drained control acid amides. [12][13][14] The third one is an ATP-dependent rats or EHBR was studied. Biliary excretion of E 2 17G organic anion carrier, 15-17 and a putative carrier was and estradiol metabolites in EHBR was markedly delayed. Analyses of biliary metabolites after estradiol in-recently reported by Pikula et al. 18,19 The genetic defect jection showed less polar conjugates in EHBR. In conin mutant hyperbilirubinemic rats, Tr 0 and GY rats 20,21 trast, the excretion of taurocholate and vinblastine and EHBR, 22 is considered to be an abnormality of the (VLB) was only slightly delayed in EHBR. Although phecanalicular organic anion carrier. 17,23 Furthermore, renothiazine treatment to induce the expression of P-GP cent studies suggest the existence of two or more transincreased biliary vinblastine excretion, it did not affect port systems for organic anions at the canalicular membiliary excretion of a tracer dose of [ 3 H]estradiol-17bbrane. [24][25][26]