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Biochem/physiol Actions
Highly selective and high-affinity mu (μ) opioid receptor (MOR) antagonist in vitro and in vivo.
NAQ is a highly selective and high-affinity mu (μ) opioid receptor (MOR) antagonist with 241- & 48-fold selectivity over the delta (δ) and kappa (κ) opioid receptor, respectively (MOR/DOR/KOR Ki = 0.55/132.5/26.45 nM) and little MOR agonist activity (Emax = 15.83% of that of DAMGO by GTP[γS] binding using membrane from MOR-expressing cells). NAQ effectively antagonizes morphine antinociceptive effects in mice in vivo (warm-water tail immersion test AD50 = 0.45 mg/kg s.c. 5 min prior to 10 mg morphine/kg s.c.; no agonist efficacy up to 100 mg/kg).
Disclaimer
Hygroscopic
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| storage condition | desiccated |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | 2-8°C |
| SMILES string | O[C@]12[C@@]34C5=C(C[C@H]2N(CC4)CC6CC6)C=CC(O)=C5O[C@@]3([H])[C@H](CC1)NC(C7=CC8=C(C=CC=C8)C=N7)=O.[2HCl] |
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