L503F variant of carnitine/organic cation transporter 1 efficiently transports metformin and other biguanides

• Published in: Journal of pharmacy and pharmacology Vol. 68; no. 9; p. 1160
• Main Authors: Futatsugi, Azusa, Masuo, Yusuke, Kawabata, Shiori, Nakamichi, Noritaka, Kato, Yukio
• Format: Journal Article
• Language: English
• Published: England 01.09.2016
• Subjects: Amines - metabolism; Amines - pharmacokinetics; Asian Continental Ancestry Group; Biguanides - metabolism; Biguanides - pharmacokinetics; Biological Transport, Active; Buformin - metabolism; Buformin - pharmacokinetics; Carnitine - metabolism; Cyclohexanecarboxylic Acids - metabolism; Cyclohexanecarboxylic Acids - pharmacokinetics; Ergothioneine - metabolism; Ergothioneine - pharmacokinetics; European Continental Ancestry Group; gamma-Aminobutyric Acid - metabolism; gamma-Aminobutyric Acid - pharmacokinetics; HEK293 Cells; Humans; Intestinal Absorption; Metformin - metabolism; Metformin - pharmacokinetics; Organic Cation Transporter 1 - genetics; Organic Cation Transporter 1 - metabolism; Polymorphism, Single Nucleotide; biguanide; metformin; single nucleotide polymorphism; cytotoxicity; organic cation transporter

Carnitine/organic cation transporter 1 (OCTN1) is involved in gastrointestinal absorption and mitochondrial toxicity of biguanides in rodents, but its pharmacokinetic roles in humans are largely unknown. The purpose of this study was to clarify the transport activities of two major OCTN1 variants, L...