Naloxone HCl

For research use only.

Catalog No.S3066

4 publications

Naloxone HCl Chemical Structure

CAS No. 357-08-4

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

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10mM (1mL in DMSO) EUR 127 In stock
EUR 95 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

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Chemical Information

Molecular Weight 363.84


CAS No. 357-08-4
Storage powder
in solvent
Synonyms N/A
Smiles C=CCN1CCC23C4C(=O)CCC2(C1CC5=C3C(=C(C=C5)O)O4)O.Cl

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04295135 Recruiting Behavioral: Chronic Pain OneSheet Chronic Pain Indiana University|Eskenazi Health|Wake Forest University|Wake Forest University Health Sciences|University of Florida August 4 2020 Not Applicable
NCT04129138 Recruiting Other: Survey Administration Caregiver|Patient M.D. Anderson Cancer Center|National Cancer Institute (NCI) July 18 2020 --
NCT04427202 Not yet recruiting Behavioral: Referral to harm reduction services HIV|Hepatitis C|Opioid-use Disorder|Injection Drug Use University of Chicago|Southern Illinois University|The Community Action Place Inc.|New York University|University of Illinois at Chicago|University of Washington|National Institute on Drug Abuse (NIDA) July 2020 Not Applicable
NCT04398316 Not yet recruiting Drug: Lidocaine Iv|Drug: HYDROmorphone Injection Abdominal Pain|Renal Colic Hennepin Healthcare Research Institute July 2020 Phase 4
NCT04234191 Not yet recruiting Drug: Buprenorphine/naloxone|Drug: Hydromorphone Opioid Use Disorder University of British Columbia|Vancouver Coastal Health April 2020 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID