In vivo visualization and quantification of (disturbed) Oatp-mediated hepatic uptake and Mrp2-mediated biliary excretion of 99mTc- mebrofenin in mice

Journal of Nuclear Medicine

Volumn 54, Issue 4, 2013, Pages 624-630

  Neyt, Sara ^a   Huisman, Maarten T ^b   Vanhove, Christian ^a   De Man, Hilde ^b   Vliegen, Maarten ^b   Moerman, Lieselotte ^a   Dumolyn, Caroline ^a   Mannens, Geert ^b   De Vos, Filip ^a  

^a GHENT UNIVERSITY   (Belgium)

^b JANSSEN RESEARCH AND DEVELOPMENT   (Belgium)

Author keywords

99mTc mebrofenin; Hepatobiliary transport; Mrp2; Oatp1a 1b; Smallanimal SPECT

Indexed keywords

MEBROFENIN TC 99M; MULTIDRUG RESISTANCE PROTEIN 2; ORGANIC ANION TRANSPORTER 1; ORGANIC ANION TRANSPORTER 1A; ORGANIC ANION TRANSPORTER 1B; RIFAMPICIN; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; BILIARY EXCRETION; BLOOD SAMPLING; CONTROLLED STUDY; CORRELATION ANALYSIS; DRUG DISTRIBUTION; DRUG EXCRETION; DRUG UPTAKE; ENZYME ACTIVITY; ENZYME INHIBITION; FEMALE; FRIEND LEUKEMIA VIRUS; IMAGE PROCESSING; IN VIVO STUDY; INTESTINE; INTRAHEPATIC CHOLESTASIS; LIVER; LIVER CLEARANCE; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN FUNCTION; QUANTITATIVE ANALYSIS; SINGLE PHOTON EMISSION COMPUTER TOMOGRAPHY;

ANIMALS; BILE DUCTS; BIOLOGICAL TRANSPORT; CHO CELLS; CRICETINAE; CRICETULUS; DOSE-RESPONSE RELATIONSHIP, DRUG; FEMALE; IMINO ACIDS; LIGATION; LIVER; MICE; ORGANIC ANION TRANSPORT PROTEIN 1; ORGANIC ANION TRANSPORTERS, SODIUM-INDEPENDENT; ORGANIC CATION TRANSPORTER 1; ORGANOTECHNETIUM COMPOUNDS; P-GLYCOPROTEINS; RIFAMPIN; TOMOGRAPHY, EMISSION-COMPUTED, SINGLE-PHOTON;

EID: 84875790687     PISSN: 01615505     EISSN: None     Source Type: Journal    
DOI: 10.2967/jnumed.112.108233     Document Type: Article

References (21)

1. 99mTc-HIDA cholescintigraphy in children with Dubin-Johnson syndrome. J Pediatr Gastroenterol Nutr. 1983;2: 311-312.
2. Newell SM, Graham JP, Roberts GD, et al. Quantitative hepatobiliary scintigraphy in normal cats and in cats with experimental cholangiohepatitis. Vet Radiol Ultrasound. 2001;42:70-76.
3. 99m Tc-mebrofenin in healthy horses. J Vet Intern Med. 2005;19:751-755.
4. 99m mebrofenin as a clinical probe to assess altered hepatobiliary transport: integration of in vitro, pharmacokinetic modeling, and simulation studies. Pharm Res. 2008;25: 1851-1860.
5. Nies AT, Keppler D. The apical conjugate efflux pump ABCC2 (MRP2). Pflugers Arch. 2007;453:643-659.
6. Kullak-Ublick GA, Stieger B, Hagenbuch B, Meier PJ. Hepatic transport of bile salts. Semin Liver Dis. 2000;20:273-292.
7. Wolkoff AW, Cohen DE. Bile acid regulation of hepatic physiology: hepatocyte transport of bile acids. Am J Physiol Gastrointest Liver Physiol. 2003;284:G175-G179.
8. Shitara Y, Sato H, Sugiyama Y. Evaluation of drug-drug interaction in the hepatobiliary and renal transport of drugs. Annu Rev Pharmacol Toxicol. 2005; 45:689-723.
9. Maddrey WC. Drug-induced hepatotoxicity. J Clin Gastroenterol. 2005;39 (suppl):S83-S89.
10. Padda MS, Sanchez M, Akhtar AJ, Boyer JL. Drug-induced cholestasis. Hepatology. 2011;53:1377-1387.
11. Alrefai WA, Gill RK. Bile acid transporters: structure, function, regulation and pathophysiological implications. Pharm Res. 2007;24:1803-1823.
12. Stieger B, Geier A. Genetic variations of bile salt transporters as predisposing factors for drug-induced cholestasis, intrahepatic cholestasis of pregnancy and therapeutic response of viral hepatitis. Expert Opin Drug Metab Toxicol. 2011; 7:411-425.
13. 99mTc-mebrofenin and indocyanine green. J Hepatol. 2011;54: 738-745.
14. van de Steeg E, Wagenaar E, van der Kruijssen CMM, et al. Organic anion transporting polypeptide 1a/1b-knockout mice provide insights into hepatic handling of bilirubin, bile acids, and drugs. J Clin Invest. 2010;120:2942-2952.
15. Lengyel G, Veres Z, Tugyi R, et al. Modulation of sinusoidal and canalicular elimination of bilirubin-glucoronides by rifampicin and other cholestatic drugs in a sandwich culture of rat hepatocytes. Hepatol Res. 2008;38:300-309.
16. Kosters A, Karpen SJ. Bile acid transporters in health and disease. Xenobiotica. 2008;38:1043-1071.
17. Kullak-Ublick GA, Beuers U, Paumgartner G. Hepatobiliary transport. J Hepatol. 2000;32:3-18.
18. Vlaming ML, Mohrmann K, Wagenaar E, et al. Carcinogen and anticancer drug transport by Mrp2 in vivo: studies usingMrp2 (Abcc2) knockout mice. J Pharmacol Exp Ther. 2006;318:319-327.
19. 99m IDA complexes. Appl Radiat Isot. 2004;61:1151-1155.
20. Vavricka SR, Van Montfoort J, Riem Ha H, Meier PJ, Fattinger K. Hepatology. 2002;36:164-172.
21. Mita S, Suzuki H, Akita H, et al. Inhibition of bile acid transport across Na1/taurocholate cotransporting polypeptide (SLC10A1) and bile salt export pump (ABCB 11)-coexpressing LLC-PK1 cells by cholestasis-inducing drugs. Drug Metab Dispos. 2006;34:1575-1581.