Naloxone HCl

For research use only. Not for use in humans.

Catalog No.S3066

2 publications

Naloxone HCl Chemical Structure

Molecular Weight(MW): 363.84

Naloxone HCl is an opioid inverse agonist drug used to counter the effects of opiate overdose.

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10mM (1mL in DMSO) USD 130 In stock
USD 97 In stock
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Biological Activity

Description Naloxone HCl is an opioid inverse agonist drug used to counter the effects of opiate overdose.
Opioid receptor [1]
In vitro

Naloxone significantly reduces the LPS-induced degeneration of the midbrain neurons. Naloxone inactives stereoisomer (+)-naloxone protected the dopaminergic neurons with equal potency. Naloxone inhibits LPS-induced activation of microglia and release of proinflammatory factors, and inhibition of microglia generation of superoxide free radical best correlated with the neuroprotective effect of naloxone isomers. Naloxone is found to partially inhibit the binding of [(3)H]LPS to cell membranes, whereas it failes to prevent damage to dopaminergic neurons by peroxynitrite, a product of nitric oxide and superoxide. [1] Naloxone (18.0 mg/kg) suppresses water intake when water is presented as the sole source of fluid. Naloxone produces a dose-dependent decrease in ethanol consumption, without altering water intake, when rats are given a free-choice between the ethanol solution and water. [2]

In vivo Naloxone (10 mg/kg) causes a dose-dependent reduction of break-points and locomotor activity in both the beer and near-beer rats. [3] Naloxone inhibits the LPS-induced activation of microglia and significantly reduces the LPS-induced loss of dopaminergic neurons in the rat substantia nigral. [4] Naloxone abolishes this antinociceptive activity both in the hot-plate test and in the first phase of the formalin test without affecting the serum concentration of paracetamol. Naloxone prevents the increase in 5-HT concentration in the central nervous system and the reduction in 5-HT2 receptors in cortical membranes. [5]


Solubility (25°C)

In vitro DMSO 72 mg/mL (197.88 mM)
Water 72 mg/mL (197.88 mM)
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 363.84


CAS No. 357-08-4
Storage powder
in solvent
Synonyms N/A
Smiles Cl.OC1=C2OC3C(=O)CCC4(O)C5CC(=C2C34CCN5CC=C)C=C1

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04111939 Not yet recruiting Other: Communities That HEAL|Other: Wait-list control Opioid Use Disorder (OUD) RTI International|Boston Medical Center|Columbia University|Ohio State University|University of Kentucky|National Institute on Drug Abuse (NIDA)|Substance Abuse and Mental Health Services Administration (SAMHSA) December 1 2019 Not Applicable
NCT04051619 Recruiting Drug: intranasal oxytocin 40 IU twice a day for 7 days Opioid Use Disorder Brown University August 2019 Phase 1
NCT03545321 Recruiting Behavioral: MOON+ Pharmacies|Opioid Use|Patient Safety Boston Medical Center|Comagine Health|Oregon Health and Science University|University of Rhode Island|University of Washington|National Institute on Drug Abuse (NIDA) July 9 2019 Not Applicable
NCT04099719 Active not recruiting -- Drug Use NHS Tayside July 1 2019 --

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID