2. Membrane Transporter/Ion Channel Neuronal Signaling GPCR/G Protein
  3. GlyT 5-HT Receptor Serotonin Transporter
  4. 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.

RPI-GLYT2-82

RPI-GLYT2-82 Chemical Structure

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RPI-GLYT2-82 Related Antibodies

Top Publications Citing Use of Products

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GlyT1 GlyT2

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5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

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Description

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[1].

IC50 & Target[1]

GlyT2

544 nM (IC50)

5-HT2A Receptor

1.9 μM (IC50)

In Vivo

RPI-GLYT2-82 (50-150 mg/kg, i.p., single administration) produces dose-dependent analgesic effects in mouse chronic constriction injury (CCI) and partial sciatic nerve ligation (PSNL) neuropathic pain models[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 (male, female, 6 weeks old at arrival); C57BL/6J (male, 8-12 weeks old, conditioned place preference model)[1]
Dosage: 50 mg/kg; 100 mg/kg; 250 mg/kg; 150 mg/kg (CPP)
Administration: i.p.; single dose
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
Molecular Weight

443.97

Formula

C24H30ClN3O3
SMILES

O=C(C1=CC2=C(N(C(C3=CC=CC=C3)=O)CC2)C=C1)NCC4(N(C)C)CCOCC4.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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RPI-GLYT2-82 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RPI-GLYT2-82GlyT5-HT ReceptorSerotonin TransporterGlycine transportersSerotonin Receptor5-hydroxytryptamine Receptor5-HTTSERTSLC6A4mouse CCI neuropathic pain model5-HT2A receptormouse PSNL neuropathic pain modelhGlyT2Δ185blood-brain barrierhGlyT2WTGlyT2neuropathic painallodyniaInhibitorinhibitorinhibit

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HY-181977
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