Naloxone

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

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Naloxone Chemical Structure

CAS No. : 465-65-6

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Other Forms of Naloxone:

Naloxone-d₅ Get quote
Naloxone hydrochloride Get quote
Naloxone hydrochloride dihydrate Get quote
Naloxone (Standard) Get quote

2 Publications Citing Use of MCE Naloxone

Proliferation Assay

: 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.

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•Related Small Molecules:

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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.

Molecular Weight

327.37

Formula

C₁₉H₂₁NO₄

CAS No.

465-65-6

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

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. McIntosh TK, et al. Beneficial effect of the nonselective opiate antagonist naloxone hydrochloride and the thyrotropin-releasing hormone (TRH) analog YM-14673 on long-term neurobehavioral outcome following experimental brain injury in the rat. J Neurotrau [Content Brief]

[2]. Sun L, et al. Endocannabinoid activation of CB1 receptors contributes to long-lasting reversal of neuropathic pain by repetitive spinal cord stimulation. Eur J Pain. 2017 May;21(5):804-814. [Content Brief]

[3]. Izquierdo I, et al. Effect of ACTH, epinephrine, beta-endorphin, naloxone, and of the combination of naloxone or beta-endorphinwith ACTH or epinephrine on memory consolidation. Psychoneuroendocrinology. 1983;8(1):81-7. [Content Brief]

[4]. Soteropoulos GC, et al. Neuromuscular effects of morphine and naloxone. J Pharmacol Exp Ther. 1973 Jan;184(1):136-42. [Content Brief]

Naloxone Related Classifications

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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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