2. GPCR/G Protein Neuronal Signaling
  3. Opioid Receptor
  4. Naloxone

Naloxone  (Synonyms: 纳洛酮)

目录号: HY-17417A
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摩尔计算器

Naloxone 是 Opioid receptor 的拮抗剂。Naloxone 可减轻阿片类药物过量引起的呼吸抑制。Naloxone 可能会引起肺水肿和心律失常。

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Naloxone Chemical Structure

Naloxone Chemical Structure

CAS No. : 465-65-6

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Naloxone 的其他形式现货产品:

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Naloxone 相关抗体

Top Publications Citing Use of Products
Proliferation Assay

    Naloxone purchased from MCE. Usage Cited in: Eur J Pain. 2017 May;21(5):804-814.  [Abstract]

    The SCS1 (early SCS)-mediated increase in the ipsilateral:contralateral PWT ratio (compared to pre-SCS) is significantly reduced by the opioid receptor antagonist, Naloxone, which is administered 10 min before SCS1.

    查看 Opioid Receptor 亚型特异性产品:

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    μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Naloxone is an antagonist of Opioid receptor. Naloxone alleviates opioid-overdose-induced respiratory depression. Naloxone may cause pulmonary edema and cardiac arrhythmias[1].

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    CHO IC50
    146 nM
    Compound: Naloxone
    Antagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding incubated for 1 hr
    Antagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding incubated for 1 hr
    		[PMID: 30996778]
    CHO IC50
    15.37 nM
    Compound: 3; NLX
    Antagonist activity at mouse mu opioid receptor expressed in CHO cells cotransfected with Galphaqi5 assessed as inhibition of DAMGO-induced increase in intracellular calcium concentration preincubated for 60 mins in Fluo4AM solution followed by compound a
    Antagonist activity at mouse mu opioid receptor expressed in CHO cells cotransfected with Galphaqi5 assessed as inhibition of DAMGO-induced increase in intracellular calcium concentration preincubated for 60 mins in Fluo4AM solution followed by compound a
    		[PMID: 31782922]
    CHO IC50
    153 nM
    Compound: Naloxone
    Antagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding preincubated for 5 mins followed by SNC80 addition and measured after 1 hr
    Antagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding preincubated for 5 mins followed by SNC80 addition and measured after 1 hr
    		[PMID: 32530286]
    CHO IC50
    78.2 nM
    Compound: Naloxone
    Antagonist activity at human DOR expressed in CHO cell membranes assessed as reduction in SNC80-induced response incubated for 1 hr by [35S]-GTPgammaS coupling assay
    Antagonist activity at human DOR expressed in CHO cell membranes assessed as reduction in SNC80-induced response incubated for 1 hr by [35S]-GTPgammaS coupling assay
    		[PMID: 31834798]
    HEK-293T IC50
    0.045 μM
    Compound: Naloxone
    Antagonist activity at recombinant human MOR expressed in HEK293T cells assessed as reduction in DAMGO-induced inhibition of forskolin-stimulated cAMP level preincubated for 15 to 20 mins followed by DAMGO and forskolin addition by GloSensor assay
    Antagonist activity at recombinant human MOR expressed in HEK293T cells assessed as reduction in DAMGO-induced inhibition of forskolin-stimulated cAMP level preincubated for 15 to 20 mins followed by DAMGO and forskolin addition by GloSensor assay
    		[PMID: 28726402]
    体内研究
    (In Vivo)

    Naloxone (2.0 mg/kg with constant infusion of 1.7 mg/kg/h) causes a significant improvement in neurobehavioral outcome which persists up to 4 weeks postinjury in rat. Naloxone treatment causes a modest and nonsignificant increase in mean arterial blood pressure (MAP)[1]. Naloxone (0.4 mg/kg) causes memory facilitation and antagonizes the amnestic effect of ACTH and epinephrine in rat[2]. Naloxone treatment diminishes the strength of the initial tetanus in a dose-related manner in cats. Naloxone (5 or 10 mg/kg, i.v.) causes subsequent doses of morphine to produce less PTP depression but has no effect on maximal twitch depression[3].

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

    327.37

    Formula

    C19H21NO4
    CAS 号
    中文名称

    纳洛酮
    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.
    纯度 & 产品资料
    参考文献

    Naloxone 相关分类

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Naloxone465-65-6纳洛酮Opioid ReceptorOpioid receptor antagonistμ-opioid-receptorPulmonary edemaCardiac arrhythmias.Inhibitorinhibitorinhibit

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