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Muopioid receptor antagonist9 is a potent and highly selective μ-opioid receptor (MOR) antagonist with the ability to cross the blood-brain barrier, having a Ki value of 77.3 nM. It exhibits selectivity for the κ-opioid receptor (KOR) and δ-opioid receptor (DOR). This compound effectively blocks the analgesic effects of psychoactive substances and can reverse respiration depression induced by these substances in mice. Additionally, Muopioid receptor antagonist9 is applicable for research on opioid use disorder (OUD).
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | Muopioid receptor antagonist9 is a potent and highly selective μ-opioid receptor (MOR) antagonist with the ability to cross the blood-brain barrier, having a Ki value of 77.3 nM. It exhibits selectivity for the κ-opioid receptor (KOR) and δ-opioid receptor (DOR). This compound effectively blocks the analgesic effects of psychoactive substances and can reverse respiration depression induced by these substances in mice. Additionally, Muopioid receptor antagonist9 is applicable for research on opioid use disorder (OUD). |
| Targets&IC50 | μ Opioid Receptor/MOR:77.3 nM (Ki) |
| In vitro | Mu opioid receptor antagonist 9 (compound 53) inhibits calcium influx induced by DAMGO and psychoactive substances in mMOR-CHO cells, with IC50 values of 33.6 μM and 4.51 μM, respectively. |
| In vivo | Mu opioid receptor antagonist 9 (1-10 mg/kg; subcutaneous injection; single dose) can inhibit the analgesic effect of psychoactive substances in the warm-water tail immersion pain model in mice. Additionally, when administered subcutaneously at doses of 1-32 mg/kg, 20 minutes post-psychoactive substance administration, it effectively reverses respiration depression induced by psychoactive substances in mice, as demonstrated in whole-body plethysmography studies. |
| Molecular Weight | 374.91 |
| Formula | C21H27ClN2O2 |
| Cas No. | 3058600-77-1 |
| Smiles | Cl.O=C(C1=COC=C1)N(C=2C=CC=CC2)C3CCCN(CC=C)CCC3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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