Cat. No.: HY-17417B

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Naloxone hydrochloride dihydrate

Name: Naloxone hydrochloride dihydrate
Brand: MedChemExpress
SKU: HY-17417B
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8 Cited Publications

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Based on 8 publication(s) in Google Scholar

Naloxone hydrochloride is an orally active opioid receptor antagonist. Naloxone hydrochloride attenuates spinal cord stimulation‑associated anti‑hyperalgesic effects, antagonizes physiologic effects of endogenous opioid peptides linked to central nervous system injury sequelae, functions as a pressor agent to induce modest elevations in mean arterial blood pressure, exerts neuroprotective effects to improve post‑traumatic neurologic motor function, blocks opioid receptor‑mediated amnesic pathways, enhances memory consolidation, reverses Adrenocorticotropic hormone (ACTH) (HY-106373)‑ and epinephrine‑induced amnesia, and potentiates the memory‑facilitatory effects of ACTH and epinephrine.

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

CAS No.: 51481-60-8
Formula: C₁₉H₂₆ClNO₆
Molecular Weight:399.87

Storage:

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

Data Sheet (302 KB)

Naloxone hydrochloride dihydrate Chemical Structure

CAS No.: 51481-60-8

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Publications (8)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

All Opioid Receptor Isoforms :

In Vitro

Naloxone (800 µg per tablet; 2 h annealing, 5 days freeze drying) hydrochloride forms freeze-dried buccal tablets that form a stable amorphous matrix that remains chemically and physically intact for 9 months at 4°C or 25°C^[4].
Naloxone (800 µg per tablet; up to 30 s) hydrochloride forms freeze-dried buccal tablets that achieve 90% disintegration in 4.8 seconds under buccal-relevant conditions (37°C, 0.7 mL phosphate buffer) and fully disintegrate within 30 s across all tested temperature and medium volume conditions^[4].

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

In Vivo

Naloxone (10 mg/kg; i.p.; single dose) hydrochloride significantly inhibits the early SCS-induced reversal of neuropathic mechanical hypersensitivity in male Sprague Dawley rats, but has no effect on the incremental anti-hyperalgesic effect of late SCS^[1].
Naloxone (2.0 mg/kg; 1.7 mg/kg/h; i.v.; bolus over 60 seconds followed by constant infusion; 4 hours) hydrochloride significantly improves long-term neurologic motor recovery up to 4 weeks following moderate fluid-percussion traumatic brain injury in male Sprague-Dawley rats, with a median composite neurologic score of 18.5 at week 4^[2].
Naloxone (0.4 mg/kg; i.p.; single immediate post-training injection) hydrochloride produces significant memory facilitation in male Wistar rats trained on task 1 and 2, and reverses the amnesic effects of post-training Adrenocorticotropic hormone (ACTH) (HY-106373) and epinephrine administration^[3].

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

Animal Model:

Sprague Dawley (adult male, 200-250 g, neuropathic pain model via partial sciatic nerve ligation and epidural monopolar electrode implantation at spinal segments T12/13)^[1]
Dosage:

10 mg/kg
Administration:

i.p.; single dose
Result:

Decreased the ipsilateral:contralateral paw withdrawal threshold ratio after SCS1.
Exerted no discernible effect on the anti-hyperalgesic effect induced by SCS2.

Animal Model:

Sprague-Dawley (male, moderate severity lateral fluid-percussion traumatic brain injury induced via 2.4 to 2.5 atmosphere pressure pulse)^[2]
Dosage:

2.0 mg/kg (bolus); 1.7 mg/kg/h (infusion)
Administration:

i.v.; bolus over 60 seconds followed by constant infusion; 4 hours
Result:

Caused a modest, nonsignificant increase in mean arterial blood pressure during 4-hour postinjury monitoring period.
Showed no significant changes to arterial blood gases, pH, or brain temperature.
Exhibited no significant improvement in composite neurologic motor scores at 24 hours postinjury.
Achieved a significant improvement in median composite neurologic motor scores at 1 week postinjury.
Reached a median composite neurologic motor score of 18.5 out of maximum 20 by week 4.
Resulted in 100% survival rate over the 4-week study period.

Animal Model:

Wistar rats (male, age 51-69 days, weight 140-200 g, step-down inhibitory avoidance task 1 training)^[3]
Dosage:

0.4 mg/kg
Administration:

i.p.; single immediate post-training injection
Result:

Produced a median (mean) training-test step-down latency difference of 180.00 sec.
Produced a median (mean) training-test step-down latency difference of 180.00 (144.45) sec when co-administered with 2.0 μg/kg ACTH_1-24, reversing the amnesic effect of ACTH alone and showing a significant difference from naloxone alone.
Produced a median (mean) training-test step-down latency difference of 180.00 (134.98) sec when co-administered with 50.0 μg/kg epinephrine HC1, reversing the amnesic effect of epinephrine alone and showing a significant difference from naloxone alone.

Animal Model:

Wistar rats (male, age 51-69 days, weight 140-200 g, step-down inhibitory avoidance task 2 training)^[3]
Dosage:

0.4 mg/kg
Administration:

i.p.; single immediate post-training injection
Result:

Produced a median (mean) training-test step-down latency difference of 24.13 (56.18) sec, showing significant memory facilitation compared to saline controls.
Produced a median (mean) training-test step-down latency difference of 105.07 (113.65) sec when co-administered with 2.0 μg/kg ACTH_1-24, potentiating the facilitatory effect of ACTH alone and showing a significant difference from naloxone alone .
Produced a median (mean) training-test step-down latency difference of 81.85 (96.86) sec when co-administered with 50.0 μg/kg epinephrine HC1, potentiating the facilitatory effect of epinephrine alone and showing a significant difference from naloxone alone.

Chemical Information

CAS No. 51481-60-8
Molecular Weight 399.87
Formula C₁₉H₂₆ClNO₆
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

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

Publications (8)

All OthersCell Proliferation/Viability Assay

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Journal Impact Factor

Nature

Structural snapshots capture nucleotide release at the μ-opioid receptor. [Abstract]

2025 Dec;648(8094):755-763. PMID: 41193810
Nat Methods

Single-molecule localization and diffusivity microscopy reveals dynamic biomolecular organization in living cells. [Abstract]

2026 May;23(5):1011-1023. PMID: 42050111
Nat Commun

Neuropeptide Y neurons mediate opioid-induced itch by disinhibiting GRP-GRPR microcircuits in the spinal cord. [Abstract]

2025 Aug 1;16(1):7074. PMID: 40750771

Naloxone hydrochloride dihydrate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Aug 1;16(1):7074. [Abstract]

Heatmaps shows the calcium signals within the 10-25 min after drugs injection (i.t., 0.3 nmol Morphine, 10 nmol Naloxone + 0.3 nmol Morphine, and 10 μg NPY + 0.3 nmol Morphine), n = 5 mice per group.
Cell Rep

Morphine and Naloxone Facilitate Neural Stem Cells Proliferation via a TET1-Dependent and Receptor-Independent Pathway. [Abstract]

2020 Mar 17;30(11):3625-3631.e6. PMID: 32187535

Naloxone hydrochloride dihydrate purchased from MedChemExpress. Usage Cited in: Cell Rep. 2020 Mar 17;30(11):3625-3631.e6. [Abstract]

NSCs were treated with different concentrations of Naloxone, Morphine, Naloxone and Morphine (Mor+Nal, 1:1), or Nal-M. Cell numbers were determined on day 3.

Naloxone hydrochloride dihydrate purchased from MedChemExpress. Usage Cited in: Cell Rep. 2020 Mar 17;30(11):3625-3631.e6. [Abstract]

Neural stem cells (NSCs) were treated with 1 μM Naloxone or Morphine. The contents of 5mC and 5hmC in NSCs (day 3) were determined by high-spot Western blot assay.
Br J Pharmacol

Semax peptide targets the μ opioid receptor gene Oprm1 to promote deubiquitination and functional recovery after spinal cord injury in female mice. [Abstract]

2025 Jul 21. PMID: 40692165
J Med Chem

2026 Mar 5;69(6):6508-6527.
Eur J Pain

Endocannabinoid activation of CB1 receptors contributes to long-lasting reversal of neuropathic pain by repetitive spinal cord stimulation. [Abstract]

2017 May;21(5):804-814. PMID: 28107590

Naloxone hydrochloride dihydrate 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.
bioRxiv

2026 Jun 3.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (302 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Sun L, et al. Endocannabinoid activation of CB receptors contributes to long-lasting reversal of neuropathic pain by repetitive spinal cord stimulation. European journal of pain (London, England). 2017 May;21(5):804-814. [Content Brief]

[2]. 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 Neurotrauma. 1993 Winter;10(4):373-84.
[Content Brief]

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

[4]. Alqurshi A, et al. Amorphous Formulation and in Vitro Performance Testing of Instantly Disintegrating Buccal Tablets for the Emergency Delivery of Naloxone. Molecular pharmaceutics. 2016 May 02;13(5):1688-98.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Naloxone hydrochloride dihydrate

8 Cited Publications

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Naloxone hydrochloride dihydrate

Publications Citing Use of MedChemExpress (MCE) Naloxone hydrochloride dihydrate

All Opioid Receptor Isoforms

Biological Activity

Chemical Information

Publications (8)

Purity & Documentation

References

Calculators

Help & FAQs

Naloxone hydrochloride dihydrate Related Classifications

HY-17417B Related Classifications

Bioz