Biomaterial Database

Effects of organic anions and bile acid conjugates on biliary excretion of pravastatin in the rat. 1998

S Fukumura, and H Takikawa, and M Yamanaka

Department of Medicine, Teikyo University School of Medicine, Tokyo, Japan.

OBJECTIVE Biliary organic anion excretion is mediated by an ATP-dependent primary active transporter, a so-called canalicular multispecific organic anion transporter (cMOAT). As there appear to be many canalicular organic anion transports, we examined the effects of various organic anions and bile acid conjugates on the biliary excretion of pravastatin in rats. METHODS [14C]pravastatin was intravenously injected into rats with bile drainage in the presence and absence of the continuous infusion of organic anions and bile acids, and radioactivity of its biliary excretion was studied. RESULTS Biliary excretion of [14C]pravastatin was markedly inhibited by sulfobromophthalein-glutathione, taurolithocholate-3-sulfate, ursodeoxycholate-3, 7-sulfate, and ursodeoxycholate-3-O-glucuronide. In contrast, dibromosulfophthalein only slightly inhibited biliary pravastatin excretion, and cefpiramide did not affect biliary pravastatin excretion. CONCLUSIONS These findings further support the multiplicity of canalicular organic anion transport, and pravastatin is considered to be excreted through a canalicular transporter which is absent in EHBR in addition to through cMOAT.

UI	MeSH Term	Description	Entries
D008297	Male		Males
D002352	Carrier Proteins	Proteins that bind or transport specific substances in the blood, within the cell, or across cell membranes.	Binding Proteins,Carrier Protein,Transport Protein,Transport Proteins,Binding Protein,Protein, Carrier,Proteins, Carrier
D005965	Glucuronates	Derivatives of GLUCURONIC ACID. Included under this heading are a broad variety of acid forms, salts, esters, and amides that include the 6-carboxy glucose structure.	Glucosiduronates,Glucuronic Acids,Acids, Glucuronic
D000818	Animals	Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA.	Animal,Metazoa,Animalia
D000924	Anticholesteremic Agents	Substances used to lower plasma CHOLESTEROL levels.	Cholesterol Inhibitors,Hypocholesteremic Agents,Anticholesteremic Drugs,Anticholesteremics,Inhibitors, Cholesterol,Agents, Anticholesteremic,Agents, Hypocholesteremic,Drugs, Anticholesteremic
D001647	Bile Acids and Salts	Steroid acids and salts. The primary bile acids are derived from cholesterol in the liver and usually conjugated with glycine or taurine. The secondary bile acids are further modified by bacteria in the intestine. They play an important role in the digestion and absorption of fat. They have also been used pharmacologically, especially in the treatment of gallstones.	Bile Acid,Bile Salt,Bile Salts,Bile Acids,Acid, Bile,Acids, Bile,Salt, Bile,Salts, Bile
D001652	Bile Ducts	The channels that collect and transport the bile secretion from the BILE CANALICULI, the smallest branch of the BILIARY TRACT in the LIVER, through the bile ductules, the bile ducts out the liver, and to the GALLBLADDER for storage.	Bile Duct,Duct, Bile,Ducts, Bile
D013431	Sulfates	Inorganic salts of sulfuric acid.	Sulfate,Sulfates, Inorganic,Inorganic Sulfates
D017035	Pravastatin	An antilipemic fungal metabolite isolated from cultures of Nocardia autotrophica. It acts as a competitive inhibitor of HMG CoA reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES).	Eptastatin,Apo-Pravastatin,Bristacol,CS-514,Elisor,Lin-Pravastatin,Lipemol,Liplat,Lipostat,Mevalotin,Nu-Pravastatin,Prareduct,Pravachol,Pravacol,Pravasin,Pravastatin Monosodium Salt, (6 beta)-Isomer,Pravastatin Sodium,Pravastatin Sodium Salt,Pravastatin tert-Octylamine Salt,Pravastatin, (6 beta)-Isomer,RMS-431,SQ-31,000,SQ-31000,Selektine,Vasten,Apo Pravastatin,CS 514,CS514,Lin Pravastatin,Nu Pravastatin,Pravastatin tert Octylamine Salt,RMS 431,RMS431,SQ 31,000,SQ 31000,SQ31,000,SQ31000,Sodium Salt, Pravastatin
D017207	Rats, Sprague-Dawley	A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.	Holtzman Rat,Rats, Holtzman,Sprague-Dawley Rat,Rats, Sprague Dawley,Holtzman Rats,Rat, Holtzman,Rat, Sprague-Dawley,Sprague Dawley Rat,Sprague Dawley Rats,Sprague-Dawley Rats