RPI-GLYT2-82
RPI-GLYT2-82 is a reversible, blood-brain barrier-permeable allosteric inhibitor of GlyT2 with an IC50 value of 554 nM. RPI-GLYT2-82 also exhibits inhibitory activity against 5-HT2AR and SERT, with IC50 values of 1.9 μM and 4.7 μM, respectively. RPI-GLYT2-82 inhibits pain signals and alleviates allodynia, shows no target-related side effects at the maximum analgesic dose, and has no addictive potential. RPI-GLYT2-82 can be used for the research of neuropathic pain.
For research use only. We do not sell to patients.
- Formula: C24H30ClN3O3
- Molecular Weight:443.97
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All 5-HT Receptor Isoforms
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Biological Activity
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GlyT2 544 nM (IC50) |
5-HT2A Receptor 1.9 μM (IC50) |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, female, 6 weeks old at arrival); C57BL/6J (male, 8-12 weeks old, conditioned place preference model)[1]
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Dosage:50 mg/kg; 100 mg/kg; 250 mg/kg; 150 mg/kg (CPP)
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Administration:i.p.; single dose
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Result:Produced dose-dependent anti-hyperalgesia effect without on-target side effects at therapeutic doses (50 mg/kg, 100 mg/kg) and showed no addiction liability up to 150 mg/kg
Chemical Information
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Molecular Weight 443.97
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Formula C24H30ClN3O3
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SMILES
O=C(C1=CC2=C(N(C(C3=CC=CC=C3)=O)CC2)C=C1)NCC4(N(C)C)CCOCC4.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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