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

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

For research use only. We do not sell to patients.

Naloxone

Naloxone Chemical Structure

CAS No. : 465-65-6

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Based on 5 publication(s) in Google Scholar

Other Forms of Naloxone:

Naloxone Related Antibodies

Top Publications Citing Use of Products

    Naloxone purchased from MedChemExpress. 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.

    View All Opioid Receptor Isoform Specific Products:

    View All Isoforms
    μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    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]
    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    327.37

    Formula

    C19H21NO4
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    OC1=C(O2)C([C@]([C@]2([H])C(CC3)=O)(CCN4CC=C)[C@]3(O)[C@H]4C5)=C5C=C1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, protect from light, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (305.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.0546 mL 15.2732 mL 30.5465 mL
    5 mM 0.6109 mL 3.0546 mL 6.1093 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 5 mg/mL (15.27 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 5 mg/mL (15.27 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.0546 mL 15.2732 mL 30.5465 mL 76.3662 mL
    5 mM 0.6109 mL 3.0546 mL 6.1093 mL 15.2732 mL
    10 mM 0.3055 mL 1.5273 mL 3.0546 mL 7.6366 mL
    15 mM 0.2036 mL 1.0182 mL 2.0364 mL 5.0911 mL
    20 mM 0.1527 mL 0.7637 mL 1.5273 mL 3.8183 mL
    25 mM 0.1222 mL 0.6109 mL 1.2219 mL 3.0546 mL
    30 mM 0.1018 mL 0.5091 mL 1.0182 mL 2.5455 mL
    40 mM 0.0764 mL 0.3818 mL 0.7637 mL 1.9092 mL
    50 mM 0.0611 mL 0.3055 mL 0.6109 mL 1.5273 mL
    60 mM 0.0509 mL 0.2546 mL 0.5091 mL 1.2728 mL
    80 mM 0.0382 mL 0.1909 mL 0.3818 mL 0.9546 mL
    100 mM 0.0305 mL 0.1527 mL 0.3055 mL 0.7637 mL
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    Naloxone Related Classifications

    Help & FAQs
    • 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:

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

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