Bitopertin

SKU: orb1300465

Description

Bitopertin

Research Area

Neuroscience

Key Properties

• CAS Number: 845614-11-1
• MW: 543.46
• Purity: >99.99% (May vary between batches)
• Formula: C₂₁H₂₀F₇N₃O₄S
• SMILES: C[C@H](Oc1ccc(cc1C(=O)N1CCN(CC1)c1ncc(cc1F)C(F)(F)F)S(C)(=O)=O)C(F)(F)F
• Target: GlyT
• Solubility: H2O:Insoluble;DMSO:63.75 mg/mL (117.3 mM);Ethanol:5 mg/mL (9.2 mM)

Bioactivity

• Target IC50:
  GlyT1:25 nM
• 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.
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• In Vitro:
  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).
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• Animal Research:
  Bitopertin (RG1678) is dissolved in H2O with 0.3% Tween 80 (Mice). Bitopertin (RG1678) is prepared in Polysorbate 80, HEC, Methyl- and Propylparaben pH 6.0 (Rats).Male NMRI mice (20-30 g) are treated with Bitopertin (0.3, 3, 1, and 10 mg/kg p.o.) or vehicle (p.o.). After 1 min, L-687,414 (50 mg/kg s.c.) or vehicle is given. After 15 min of habituation in the activity chambers, horizontal activity is recorded for 60 min. The time course of Bitopertin effects on L-678,414-induced hyperactivity is also examined; locomotor activity is assessed 2.5, 4.5, and 24 h after administration of Bitopertin (L-678,414 is always given 15 min before the activity procedure). In addition, the effect of subchronic Bitopertin is investigated. Mice receive vehicle or Bitopertin (1 mg/kg p.o.) for 4 consecutive days and L-678,414-induced hyperactivity is evaluated on day 5. Wistar rats receive a 14-day treatment of PCP HC1 (5 mg/kg) or vehicle (NaCl 0.9%, 5 mL/kg i.p.). 24 h following the last injection, rats (6-18 per group) are allowed to individually habituate to the test boxes for 30 min. Rats then received Bitopertin (1, 3, 10 mg/kg p.o.) or vehicle (Polysorbate 80, HEC, Methyl- and Propylparaben pH 6.0; 5 mL/kg p.o.), followed after 1 h by 1 mg/kg D-amphetamine or vehicle i.p. Horizontal activity is recorded directly after the administration of Bitopertin until 120 min after dosing with amphetamine. Data are analyzed by ANOVA supplemented by Fischer's least significant difference post hoc test.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

RG 1678, RG-1678, RG1678, RO-4917838, RO 4917838, RO4917838, Bitopertin, inhibit, Paliflutine, Inhibitor, Glycine transporters, GlyT, GlyT1

Compound Identifiers

PubChem CID

24946690