NaQ

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NaQ

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

NAQ 是一种有效和选择性的μ阿片受体部分激动剂，K_i值为 0.55 nM。 NAQ 显示了对 δ 受体 (K_i=132.50 nM) 和 κ 受体 (K_i=26.45 nM) 的选择性。NAQ 可用于阿片类药物戒断或依赖性的研究。

生物活性

NAQ is a potent and selectiveμopioid receptorpartial agonist, with aK_iof 0.55 nM. NAQ shows selectivity for Muopioid receptorover 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].

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)

体外研究
(In Vitro)

NAQ is a μ opioid receptor (MOR) partial agonist, with an EC₅₀of 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].

体内研究
(In Vivo)

NAQ (a single s.c.) antagonizes the antinociceptive effects of Morphine in the mouse tail immersion test, with an AD₅₀of 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]

	t_1/2 (min)	V_ss (L/kg)	CL(mL/min/kg)	AUC_Inf (h·ng/mL)	T_max (min)	C_max (ng/mL)	F (%)
1 mg/kg IV	32.4	3.0	86	202	/	/	/
10 mg/kg PO	/	/	/	114	36	20	3

分子量

497.58

Formula

C₃₀H₃₁N₃O₄

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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