Naloxone HCl

Catalog No.S3066

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.

Size Price Stock Quantity  
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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02922959 Active not recruiting Drug Overdose|Opioid-Related Disorders|Drug Addiction|Drug Abuse|Substance Abuse University of Cincinnati|National Institute on Drug Abuse (NIDA) February 7 2017 Not Applicable
NCT03266445 Not yet recruiting Opioid-use Disorder|Pain Acute|Surgery Massachusetts General Hospital October 5 2018 Phase 4
NCT03687268 Recruiting Opioid-Induced Constipation Develco Pharma Schweiz AG July 31 2017 Phase 3
NCT03386591 Completed Opioid-use Disorder National Institute on Drug Abuse (NIDA) January 3 2018 Phase 1
NCT02032433 Completed Opioid Use Disorder New York University School of Medicine|National Institute on Drug Abuse (NIDA)|The EMMES Corporation January 29 2014 Phase 4
NCT03248947 Recruiting Opioid Use Disorder Duke University|National Institute on Drug Abuse (NIDA)|The EMMES Corporation March 28 2018 Early Phase 1

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Opioid Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID