Bitopertin R enantiomer, Inhibitor

Bitopertin R enantiomer

Cat. Num. AAA5752801

• Purity: 98.00%
• Synonyms: Bitopertin R enantiomer; RG1678 (R enantiomer); RO4917838 (R enantiomer); inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: <1mg/ml refers to the product slightly soluble or insoluble
• Formula: C21H20F7N3O4S
• SMILES: FC1=CC(C(F)(F)F)=CN=C1N2CCN(C(C3=CC(S(=O)(C)=O)=CC=C3O[C@@H](C(F)(F)F)C)=O)CC2
• CAS Number: 845614-12-2
• Target & IC50: GlyT1: ic50 25nM
• In Vitro: Bitopertin dose-dependently increases cerebrospinal fluid and striatal levels of glycine measured by microdialysis in rats. Additionally, Bitopertin attenuates hyperlocomotion induced by the psychostimulant D-amphetamine or thenMDA receptor glycine site antagonist L-687,414 in mice. Bitopertin also prevents the hyper-response to the D-amphetamine challenge in rats treated chronically with phencyclidine. The administration of vehicle has no effect on extracellular levels of striatal glycine, which remained constant throughout the experiment. In contrast, p.o. administration of Bitopertin (1-30mg/kg) produced a dose-dependent increase in extracellular glycine levels. Bitopertin (30mg/kg) produces glycine levels 2.5 times higher than pretreatment,levels. A similar dose-dependent increase in glycine concentration is observed in the CSF of rats treated p.o. with Bitopertin (1-10mg/kg) compared with vehicle-treated animals, 3 hours after drug administration [1]. In vivo pharmacokinetic studies in rat and monkey reveals that Bitopertin has, in both species, a low plasma clearance, an intermediate volume of distribution, a good oral bioavailability (78% for rat, 56% for monkey), and a favorable terminal half-life (5.8 h for rat, 6.4 h for monkey). The plasma protein binding is high in the two preclinical species (97%) and in human (98%). The CNS penetration of Bitopertin in rat (brain/plasma=0.7) is better than that in mouse (brain/plasma=0.5) [2].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Structure

Related Product Information for Bitopertin R enantiomer, inhibitor

Bitopertin R enantiomer (RG1678 R enantiomer) is the R-enantiomer of Bitopertin. Bitopertin is a noncompetitive glycine reuptake inhibitor and inhibits glycine uptake at human GlyT1 (IC50: 25nM).

Product Categories/Family for Bitopertin R enantiomer, inhibitor

Neuroscience; GlyT

References

Alberati D, et al. Glycine reuptake inhibitor RG1678: A pharmacologic characterization of an investigational agent for the treatment,of schizophrenia. Neuropharmacology. 2012 Feb;62(2):1152-61.
Alberati D, et al. Glycine reuptake inhibitor RG1678: A pharmacologic characterization of an investigational agent for the treatment,of schizophrenia. Neuropharmacology. 2012 Feb;62(2):1152-61.
Pinard E, et al. Selective GlyT1 Inhibitors: Discovery of [4-(3-Fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methylethoxy)phenyl]methanone (RG1678), a Promising Novel Medicine To Treat Schizophrenia. J Me
Pinard E, et al. Selective GlyT1 Inhibitors: Discovery of [4-(3-Fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methylethoxy)phenyl]methanone (RG1678), a Promising Novel Medicine To Treat Schizophrenia. J Me
Alberati, Daniela; Moreau, Jean-Luc; Lengyel, Judith et al. Glycine reuptake inhibitor RG1678: A pharmacologic characterization of an investigational agent for the treatment,of schizophrenia. Neuropharmacology (2012), 62(2), 1152-1161.
Alberati, Daniela; Moreau, Jean-Luc; Lengyel, Judith et al. Glycine reuptake inhibitor RG1678: A pharmacologic characterization of an investigational agent for the treatment,of schizophrenia. Neuropharmacology (2012), 62(2), 1152-1161.
Hofmann C, Banken L, Hahn M et al. Evaluation of the Effects of Bitopertin (RG1678) on Cardiac Repolarization: A Thorough Corrected QT Study in Healthy Male Volunteers. Clin Ther. 2012 Oct;34(10):2061-71.
Hofmann C, Banken L, Hahn M et al. Evaluation of the Effects of Bitopertin (RG1678) on Cardiac Repolarization: A Thorough Corrected QT Study in Healthy Male Volunteers. Clin Ther. 2012 Oct;34(10):2061-71.
Martin-Facklam M, Pizzagalli F, Zhou Y et al. Glycine Transporter Type 1 Occupancy by Bitopertin: a Positron Emission Tomography Study in Healthy Volunteers. Neuropsychopharmacology. 2012 Nov 7. doi: 10.1038/npp.2012.212. [Epub ahead of print]
Martin-Facklam M, Pizzagalli F, Zhou Y et al. Glycine Transporter Type 1 Occupancy by Bitopertin: a Positron Emission Tomography Study in Healthy Volunteers. Neuropsychopharmacology. 2012 Nov 7. doi: 10.1038/npp.2012.212. [Epub ahead of print]