For research use only.
Catalog No.S8219 Synonyms: RG1678, RO-4917838
CAS No. 845614-11-1
Bitopertin (RG1678,RO-4917838) is a potent inhibitor of glycine transporter 1 (GlyT1), with Ki of 8.1 nM for human hGlyT1b and IC50 of 22-25 nM in Chinese hamster ovary cells.
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|Description||Bitopertin (RG1678,RO-4917838) is a potent inhibitor of glycine transporter 1 (GlyT1), with Ki of 8.1 nM for human hGlyT1b and IC50 of 22-25 nM in Chinese hamster ovary cells.|
RG1678 noncompetitively inhibits [3H]glycine uptake in cells stably expressing hGlyT1b and mGlyT1b, with IC50 values of 25 ± 2 nM and 22 ± 5 nM, respectively (n = 6) and competitively displaces [3H]ORG24598 binding with a Ki of 8.1 nM at human hGlyT1b in membranes from Chinese hamster ovary cells. RG1678 has no effect on hGlyT2-mediated [3H]glycine uptake up to 30 μM concentration. There is no significant species difference in the pharmacology for RG1678 based on the ability of the compound to displace [3H]ORG24598. In hippocampal CA1 pyramidal cells, RG1678 enhances NMDA-dependent long-term potentiation (LTP) at 30 nM (213 ± 18%; n=7), 100 nM (269 ± 44%, n=13) but not at 300 nM (152 ± 14%; n = 9).
|In vivo||Administration of RG1678 produces a long-lasting (>3h) dose-dependent increase in extracellular glycine levels both in microdialysis experiments conducted in rats and CSF of rats. In mice, RG1678 dose-dependently and significantly attenuates hyperlocomotion induced by the psychostimulant D-amphetamine. RG1678 also prevents the hyper-response to D-amphetamine challenge in rats treated chronically with phencyclidine, an NMDA receptor open-channel blocker.|
|In vitro||DMSO||100 mg/mL (184.0 mM)|
|Ethanol||100 mg/mL (184.0 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03271541||Completed||Drug: Bitopertin||Beta-Thalassemia||Hoffmann-La Roche||October 26 2017||Phase 2|
|NCT02019290||Withdrawn||Drug: Midazolam|Drug: bitopertin||Healthy Volunteer||Hoffmann-La Roche||February 10 2014||Phase 1|
|NCT01674361||Completed||Drug: Bitopertin|Drug: Placebo|Drug: SSRI||Obsessive-Compulsive Disorder||Hoffmann-La Roche||December 31 2012||Phase 2|
|NCT01665976||Completed||Drug: RO4917838|Drug: RO4927838||Healthy Volunteer||Hoffmann-La Roche||August 2012||Phase 1|
|NCT01543529||Completed||Drug: RO4917838|Drug: Placebo to RO4917838|Other: Alcohol||Healthy Volunteer||Hoffmann-La Roche||February 28 2012||Phase 1|
|NCT01510899||Completed||Drug: RO4917838||Healthy Volunteer||Hoffmann-La Roche||October 2011||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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