Naloxone HCl

Catalog No.S3066

For research use only.

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

Naloxone HCl Chemical Structure

CAS No. 357-08-4

Selleck's Naloxone HCl has been cited by 10 Publications

Purity & Quality Control

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Biological Activity

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

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 363.84
Formula

C19H21NO4.HCl

CAS No. 357-08-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C=CCN1CCC23C4C(=O)CCC2(C1CC5=C3C(=C(C=C5)O)O4)O.Cl

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05142267 Not yet recruiting Drug: Placebo|Drug: Oxycodone|Drug: Naloxone Opioid Use Disorder|Back Pain|Stress Vanderbilt University Medical Center|National Institute on Drug Abuse (NIDA) January 2022 Not Applicable
NCT04868552 Not yet recruiting Other: Pre-hospital naloxone education Opioid Use|Pain Musculoskeletal|Surgery|Overdose of Opiate Carilion Clinic|Virginia Polytechnic Institute and State University September 2021 Not Applicable
NCT05010148 Recruiting Drug: Lidocaine IV|Drug: Placebo Postoperative Delirium|Postoperative Pain|Spinal Fusion University of California San Francisco September 17 2021 Phase 3
NCT04893525 Recruiting Drug: Buprenorphine/naloxone Opioid-use Disorder University of British Columbia July 23 2021 Phase 2|Phase 3

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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