Mu opioid receptor antagonist 7 

Mu opioid receptor antagonist 7 (compound 24) is a potent and CNS permeable antagonist of µOR (µ-opioid receptor), with an IC₅₀ of 29 ± 3.0 nM. Mu opioid receptor antagonist 7 can be used for the research of pain and opioid use disorder^[1].

Mu opioid receptor antagonist 7 (compound 24) (10 mg/kg) displays strong blockade of the analgesic effect induced by µOR agonist, demonstrating its ability to antagonize µOR agonists^[1].
Mu opioid receptor antagonist 7 (10 mg/kg, rat) can revert respiratory suppression induced by fentanyl, a higher efficacy µOR agonist^[1].
Mu opioid receptor antagonist 7 (10 mg/kg, sc, rat) can achieve 70% receptor occupancy of the µOR thus demonstrating the high CNS permeability of this compound^[1].

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

386.91

C₂₂H₂₇ClN₂O₂

2378397-30-7

OC1=CC(Cl)=C(C[C@H](N(C)C)CNC([C@@H]2C[C@]2(C)C3=CC=CC=C3)=O)C=C1

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Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Nerurkar A, et al. Novel series of tunable µOR modulators with enhanced brain penetration for the treatment of opioid use disorder, pain and neuropsychiatric indications. Bioorg Med Chem Lett. 2023 Aug 15;92:129405.  [Content Brief]