Ritu Lal, Juthamas Sukbuntherng, Ezra H L Tai, Shubhra Upadhyay, Fenmei Yao, Mark S Warren, Wendy Luo, Lin Bu, Son Nguyen, Jeanelle Zamora, Ge Peng, Tracy Dias, Ying Bao, Maria Ludwikow, Thu Phan, Randall A Scheuerman, Hui Yan, Mark Gao, Quincey Q Wu, Thamil Annamalai, Stephen P Raillard, Kerry Koller, Mark A Gallop, Kenneth C Cundy
Baclofen is a racemic GABA(B) receptor agonist that has a number of significant pharmacokinetic limitations, including a narrow window of absorption in the upper small intestine and rapid clearance from the blood. Arbaclofen placarbil is a novel transported prodrug of the pharmacologically active R-isomer of baclofen designed to be absorbed throughout the intestine by both passive and active mechanisms via the monocarboxylate type 1 transporter. Arbaclofen placarbil is rapidly converted to R-baclofen in human and animal tissues in vitro...
September 2009: Journal of Pharmacology and Experimental Therapeutics