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Namespace Prefixes

PrefixIRI
n2http://linked.opendata.cz/resource/drugbank/drug/
dctermshttp://purl.org/dc/terms/
n9http://bio2rdf.org/drugbank:
admshttp://www.w3.org/ns/adms#
rdfhttp://www.w3.org/1999/02/22-rdf-syntax-ns#
owlhttp://www.w3.org/2002/07/owl#
n3http://linked.opendata.cz/ontology/drugbank/
n4http://linked.opendata.cz/resource/drugbank/property/
xsdhhttp://www.w3.org/2001/XMLSchema#
n7http://linked.opendata.cz/resource/drugbank/drug/DB08891/identifier/drugbank/

Statements

Subject Item
n2:DB08891
rdf:type
n3:Drug
n3:description
Arbaclofen, or STX209, is the R-enantiomer of baclofen. It is believed to be a selective gamma-amino butyric acid type B receptor agonist, and has been investigated as a treatment for autism spectrum disorder and fragile X syndrome in randomized, double blind, placebo controlled trials. It has also been investigated as a treatment for spasticity due to multiple sclerosis and spinal cord injury. Arbaclofen was investigated as a treatment for gastroesophageal reflux disease (GERD); however, with disappointing results.
n3:generalReferences
1.Nance, P. W., et al. "Efficacy and safety study of arbaclofen placarbil in patients with spasticity due to spinal cord injury." Spinal cord 49.9 (2011): 974-980. 2. Lal, Ritu, et al. "Arbaclofen placarbil, a novel R-baclofen prodrug: improved absorption, distribution, metabolism, and elimination properties compared with R-baclofen." Journal of Pharmacology and Experimental Therapeutics 330.3 (2009): 911-921.
n3:group
investigational
n3:indication
Investigated in clinical trials as a potential treatment for spasticity in multiple sclerosis, autism spectrum disorder, and social withdrawal in fragile X syndrome.
owl:sameAs
n9:DB08891
dcterms:title
Arbaclofen
adms:identifier
n7:DB08891
n3:mechanismOfAction
Arbaclofen, or R-baclofen, acts upstream of the mGluR5 receptor to increase inhibitory neurotransmission. It is the isomer of baclofen which harbors antispastic activity.
n3:routeOfElimination
>80% of R-baclofen is renally eliminated unchanged.
n3:synonym
(R)-Baclofen OS440 (R)-4-Amino-3-(4-chlorophenyl)butan­oic acid STX209
n3:Water-Solubility
n4:271B5B19-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B5B1B-363D-11E5-9242-09173F13E4C5
n3:absorption
Unlike baclofen, absorption of arbaclofen is not limited to the upper small intestine. Arbaclofen can also be absorbed in the lower small intestine and the colon, allowing for the development of sustained release formulations.
n3:casRegistryNumber
69308-37-8
n3:clearance
Blood clearance of an IV bolus of R-baclofen in rats, monkeys, and dogs, resulted in a half life of 1.6-3.4hours, in one study. Total blood clearance was reported to be 0.51±0.13L/h/kg in rats, 0.31±0.11L/h/kg in monkeys, and 0.24±0.01L/h/kg in dogs. (2)
n3:Melting-Point
n4:271B5B1A-363D-11E5-9242-09173F13E4C5