FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2102955372> ?p ?o ?g. }

• W2102955372 endingPage "921" @default.
• W2102955372 startingPage "911" @default.
• W2102955372 abstract "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 <i>R</i>-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 <i>R</i>-baclofen in human and animal tissues in vitro. This conversion seems to be primarily catalyzed in human tissues by human carboxylesterase-2, a major carboxylesterase expressed at high levels in various tissues including human intestinal cells. Arbaclofen placarbil was efficiently absorbed and rapidly converted to <i>R</i>-baclofen after oral dosing in rats, dogs, and monkeys. Exposure to <i>R</i>-baclofen was proportional to arbaclofen placarbil dose, whereas exposure to intact prodrug was low. Arbaclofen placarbil demonstrated enhanced colonic absorption, i.e., 5-fold higher <i>R</i>-baclofen exposure in rats and 12-fold higher in monkeys compared with intracolonic administration of <i>R</i>-baclofen. Sustained release formulations of arbaclofen placarbil demonstrated sustained <i>R</i>-baclofen exposure in dogs with bioavailability up to 68%. In clinical use, arbaclofen placarbil may improve the treatment of patients with gastroesophageal reflux disease, spasticity, and numerous other conditions by prolonging exposure and decreasing the fluctuations in plasma levels of <i>R</i>-baclofen." @default.
• W2102955372 created "2016-06-24" @default.
• W2102955372 creator A5005526580 @default.
• W2102955372 creator A5006745126 @default.
• W2102955372 creator A5007810124 @default.
• W2102955372 creator A5012951977 @default.
• W2102955372 creator A5015312946 @default.
• W2102955372 creator A5015700210 @default.
• W2102955372 creator A5021016237 @default.
• W2102955372 creator A5021167260 @default.
• W2102955372 creator A5022302063 @default.
• W2102955372 creator A5028055236 @default.
• W2102955372 creator A5039295334 @default.
• W2102955372 creator A5046917072 @default.
• W2102955372 creator A5047505738 @default.
• W2102955372 creator A5058332617 @default.
• W2102955372 creator A5061435729 @default.
• W2102955372 creator A5063573627 @default.
• W2102955372 creator A5069840749 @default.
• W2102955372 creator A5072785251 @default.
• W2102955372 creator A5079505944 @default.
• W2102955372 creator A5080607402 @default.
• W2102955372 creator A5085787188 @default.
• W2102955372 creator A5086221395 @default.
• W2102955372 creator A5086764406 @default.
• W2102955372 creator A5087949417 @default.
• W2102955372 date "2009-06-05" @default.
• W2102955372 modified "2023-10-18" @default.
• W2102955372 title "Arbaclofen Placarbil, a Novel <i>R</i>-Baclofen Prodrug: Improved Absorption, Distribution, Metabolism, and Elimination Properties Compared with <i>R</i>-Baclofen" @default.
• W2102955372 cites W1998976350 @default.
• W2102955372 cites W2017085563 @default.
• W2102955372 cites W2017440345 @default.
• W2102955372 cites W2032586055 @default.
• W2102955372 cites W2055979252 @default.
• W2102955372 cites W2058599548 @default.
• W2102955372 cites W2060638043 @default.
• W2102955372 cites W2094149744 @default.
• W2102955372 cites W2099595411 @default.
• W2102955372 cites W2118007909 @default.
• W2102955372 cites W2122773923 @default.
• W2102955372 cites W2136934702 @default.
• W2102955372 cites W2169879202 @default.
• W2102955372 cites W2186114950 @default.
• W2102955372 cites W225048806 @default.
• W2102955372 doi "https://doi.org/10.1124/jpet.108.149773" @default.
• W2102955372 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/19502531" @default.
• W2102955372 hasPublicationYear "2009" @default.
• W2102955372 type Work @default.
• W2102955372 sameAs 2102955372 @default.
• W2102955372 citedByCount "79" @default.
• W2102955372 countsByYear W21029553722012 @default.
• W2102955372 countsByYear W21029553722013 @default.
• W2102955372 countsByYear W21029553722014 @default.
• W2102955372 countsByYear W21029553722015 @default.
• W2102955372 countsByYear W21029553722016 @default.
• W2102955372 countsByYear W21029553722017 @default.
• W2102955372 countsByYear W21029553722018 @default.
• W2102955372 countsByYear W21029553722019 @default.
• W2102955372 countsByYear W21029553722020 @default.
• W2102955372 countsByYear W21029553722021 @default.
• W2102955372 countsByYear W21029553722022 @default.
• W2102955372 countsByYear W21029553722023 @default.
• W2102955372 crossrefType "journal-article" @default.
• W2102955372 hasAuthorship W2102955372A5005526580 @default.
• W2102955372 hasAuthorship W2102955372A5006745126 @default.
• W2102955372 hasAuthorship W2102955372A5007810124 @default.
• W2102955372 hasAuthorship W2102955372A5012951977 @default.
• W2102955372 hasAuthorship W2102955372A5015312946 @default.
• W2102955372 hasAuthorship W2102955372A5015700210 @default.
• W2102955372 hasAuthorship W2102955372A5021016237 @default.
• W2102955372 hasAuthorship W2102955372A5021167260 @default.
• W2102955372 hasAuthorship W2102955372A5022302063 @default.
• W2102955372 hasAuthorship W2102955372A5028055236 @default.
• W2102955372 hasAuthorship W2102955372A5039295334 @default.
• W2102955372 hasAuthorship W2102955372A5046917072 @default.
• W2102955372 hasAuthorship W2102955372A5047505738 @default.
• W2102955372 hasAuthorship W2102955372A5058332617 @default.
• W2102955372 hasAuthorship W2102955372A5061435729 @default.
• W2102955372 hasAuthorship W2102955372A5063573627 @default.
• W2102955372 hasAuthorship W2102955372A5069840749 @default.
• W2102955372 hasAuthorship W2102955372A5072785251 @default.
• W2102955372 hasAuthorship W2102955372A5079505944 @default.
• W2102955372 hasAuthorship W2102955372A5080607402 @default.
• W2102955372 hasAuthorship W2102955372A5085787188 @default.
• W2102955372 hasAuthorship W2102955372A5086221395 @default.
• W2102955372 hasAuthorship W2102955372A5086764406 @default.
• W2102955372 hasAuthorship W2102955372A5087949417 @default.
• W2102955372 hasConcept C108215921 @default.
• W2102955372 hasConcept C110121322 @default.
• W2102955372 hasConcept C112705442 @default.
• W2102955372 hasConcept C121332964 @default.
• W2102955372 hasConcept C125287762 @default.
• W2102955372 hasConcept C134306372 @default.
• W2102955372 hasConcept C150903083 @default.
• W2102955372 hasConcept C170493617 @default.
• W2102955372 hasConcept C181199279 @default.
• W2102955372 hasConcept C181389837 @default.
• W2102955372 hasConcept C185592680 @default.

• next