About: Arbaclofen     Goto   Sponge   NotDistinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

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http://linked.open...gbank/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. (en)
http://linked.open...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. (en)
http://linked.open...gy/drugbank/group
  • investigational (en)
http://linked.open...ugbank/indication
  • Investigated in clinical trials as a potential treatment for spasticity in multiple sclerosis, autism spectrum disorder, and social withdrawal in fragile X syndrome. (en)
sameAs
Title
  • Arbaclofen (en)
adms:identifier
http://linked.open...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. (en)
http://linked.open...outeOfElimination
  • >80% of R-baclofen is renally eliminated unchanged. (en)
http://linked.open.../drugbank/synonym
  • (R)-4-Amino-3-(4-chlorophenyl)butan­oic acid (en)
  • (R)-Baclofen (en)
  • OS440 (en)
  • STX209 (en)
http://linked.open.../Water-Solubility
http://linked.open...ogy/drugbank/logP
http://linked.open...ugbank/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. (en)
http://linked.open...casRegistryNumber
  • 69308-37-8 (en)
http://linked.open...rugbank/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) (en)
http://linked.open...ank/Melting-Point
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