NAQ
NAQ is a potent and selective μ opioid receptor partial agonist, with a Ki of 0.55 nM. NAQ shows selectivity for Mu opioid receptor over the δ receptor (Ki=132.50 nM) and the κ receptor (Ki=26.45 nM). NAQ can be used for the research of opioid withdrawal or dependence.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Formel: C30H31N3O4
- Molecular Weight:497.58
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
μ Opioid Receptor/MOR 0.55 nM (Ki) |
κ Opioid Receptor/KOR 26.45 nM (Ki) |
δ Opioid Receptor/DOR 132.50 nM (Ki) |
In Vitro
NAQ is a μ opioid receptor (MOR) partial agonist, with an EC50 of 4.36 nM in MOR-expressing CHO cell line[1].
NAQ (45 min) inhibits hERG with an IC50 of 220 nM in CHO-K1 cells stably transfected with human hERG cDNA[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
NAQ (0.32-10 mg/kg; s.c.) produces weak intracranial self-stimulation (ICSS) facilitation in rats but more robust ICSS facilitation during and after Morphine treatment and also reverses Morphine withdrawal-associated depression of ICSS[2].
Pharmacokinetics of NAQ in rats[3]
| t1/2 (min) |
Vss (L/kg) |
CL(mL/min/kg) | AUCInf (h⋅ng/mL) |
Tmax (min) |
Cmax (ng/mL) |
F (%) |
|
| 1 mg/kg IV | 32.4 | 3.0 | 86 | 202 | / | / | / |
| 10 mg/kg PO | / | / | / | 114 | 36 | 20 | 3 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 497.58
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Formel C30H31N3O4
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SMILES
O=C(C1=CC2=C(C=N1)C=CC=C2)N[C@H]3[C@@H]4[C@]56C7=C(O4)C(O)=CC=C7C[C@@H](N(CC8CC8)CC6)[C@@]5(O)CC3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Li G, et, al. Design, synthesis, and biological evaluation of 6alpha- and 6beta-N-heterocyclic substituted naltrexamine derivatives as mu opioid receptor selective antagonists. J Med Chem. 2009 Mar 12;52(5):1416-27. [Content Brief]
[2]. Altarifi AA, et, al. Effects of the novel, selective and low-efficacy mu opioid receptor ligand NAQ on intracranial self-stimulation in rats. Psychopharmacology (Berl). 2015 Feb;232(4):815-24. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
NAQ Related Classifications
HY-151811 Related Classifications
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