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Merck
CN

SML3632

NAQ

≥98% (HPLC)

别名:

17-Cyclopropylmethyl-3,14b-dihydroxy-4,5a-epoxy-6a-[(3’-isoquinolyl)acetamido]morphinan dihydrochloride, N-[(5α,6α)-17-(Cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]-3-isoquinolinecarboxamide dihydrochloride

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关于此项目

经验公式(希尔记法):
C30H31N3O4·2HCl
化学文摘社编号:
分子量:
570.51
UNSPSC Code:
12352116
NACRES:
NA.21
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
Storage condition:
desiccated
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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]

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Quality Level

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

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

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历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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Megan J Moerke et al.
Neuropharmacology, 151, 180-188 (2019-03-19)
The abuse potential of opioid analgesics in humans appears to increase rapidly during initial regimens of opioid exposure. Previous work using intracranial self-stimulation (ICSS), a preclinical procedure useful for studying rewarding drug effects in drug-naïve animals, has similarly shown that
Saheem A Zaidi et al.
Bioorganic & medicinal chemistry, 21(21), 6405-6413 (2013-09-24)
Highly selective opioid receptor antagonists are essential pharmacological probes in opioid receptor structural characterization and opioid agonist functional studies. Currently, there is no highly selective, nonpeptidyl and reversible mu opioid receptor antagonist available. Among a series of naltrexamine derivatives that
Pallabi Mitra et al.
Drug metabolism and disposition: the biological fate of chemicals, 39(9), 1589-1596 (2011-06-21)
Recently, two novel N-heterocyclic derivatives of naltrexone [designated 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[(4'-pyridyl)acetamido]morphinan (NAP) and 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-[(3'-isoquinolyl) acetamido]morphinan (NAQ)] have been proposed as μ-opioid receptor (MOR) selective antagonists. The goal of this study was to examine their absorption and metabolism. The bidirectional transport of NAP
Ahmad A Altarifi et al.
Psychopharmacology, 232(4), 815-824 (2014-09-03)
Low-efficacy mu opioid receptor agonists may be useful for some clinical indications, but clinically available low-efficacy mu agonists also have low selectivity for mu vs. kappa opioid receptors. NAQ (17-cyclopropylmethyl-3,14ß-dihydroxy-4,5α-epoxy-6α-[(3'-isoquinolyl)acetamido]morphinan) is a novel opioid receptor ligand with low-efficacy at mu
Yunyun Yuan et al.
ACS chemical neuroscience, 2(7), 346-351 (2012-07-21)
As important pharmacological probes, highly selective opioid receptor antagonists are essential in opioid receptor structural characterization and opioid agonist functional studies. At present, a nonpeptidyl, highly selective, and reversible mu opioid receptor antagonist is still not available. Among a series

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