NAQ 

NAQ is a potent and selective μ opioid receptor partial agonist, with a K_i of 0.55 nM. NAQ shows selectivity for Mu opioid receptor over the δ receptor (K_i=132.50 nM) and the κ receptor (K_i=26.45 nM). NAQ can be used for the research of opioid withdrawal or dependence^[1].

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].

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

NAQ (a single s.c.) antagonizes the antinociceptive effects of Morphine in the mouse tail immersion test, with an AD₅₀ of 0.45 mg/kg^[1].
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]

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

497.58

C₃₀H₃₁N₃O₄

Room temperature in continental US; may vary elsewhere.

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

• [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]

  [3]. P. Pagare P, et, al. Preclinical Characterization and Development on NAQ as a Mu Opioid Receptor Partial Agonist for Opioid Use Disorder Treatment. ACS Pharmacol. Transl. Sci. 2022, 5, 11, 1197-1209.