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Catalog Number | orb1980124 |
---|---|
Category | Small Molecules |
Description | Tianeptine metabolite MC5, an active derivative of the atypical antidepressant tianeptine produced through β-oxidation, exhibits selective G protein activation in bioluminescence resonance energy transfer (BRET) assays. Utilizing HEK293T cells expressing the human μ-opioid receptor (MOR) over the human δ-opioid receptor (DOR; EC50s = 0.454 and > 100 µM, respectively), it demonstrates specificity. Moreover, this metabolite reduces immobility in wild-type mice during the forced swim test at a dose of 30 mg/kg, an effect not observed in MOR knockout mice, suggesting its antidepressant-like activity is MOR-dependent. |
CAS Number | 115220-11-6 |
Purity | 98.00% |
MW | 430.88 |
SMILES | O=C(CCCCNC1C2=C(N(S(=O)(C3=CC(Cl)=CC=C31)=O)C)C=CC=C2)[O-].[Na+] |
Formula | C19H20ClN2O4S.Na |
Biological Activity | Tianeptine metabolite MC5, an active derivative of the atypical antidepressant tianeptine produced through β-oxidation, exhibits selective G protein activation in bioluminescence resonance energy transfer (BRET) assays. Utilizing HEK293T cells expressing the human μ-opioid receptor (MOR) over the human δ-opioid receptor (DOR; EC50s = 0.454 and > 100 µM, respectively), it demonstrates specificity. Moreover, this metabolite reduces immobility in wild-type mice during the forced swim test at a dose of 30 mg/kg, an effect not observed in MOR knockout mice, suggesting its antidepressant-like activity is MOR-dependent. |
Storage | -20°C |
Note | For research use only |
Expiration Date | 12 months from date of receipt. |