Naltrexone (Hydrochloride) | CAS:16676-29-2

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Name:Naltrexone Hydrochloride; 
Cat. No. :CS-0763
CAS No. :16676-29-2
Formula:C20H24ClNO4
M. Wt. : 377.86
Solubility:DMSO: ≥ 33 mg/mL

Naltrexone hydrochlorideis an opioid receptor antagonist used primarily in the management of alcohol dependence and opioid dependence. IC50 Value:Target: Opioid ReceptorNaltrexone is competitive antagonist for μ, κ, δ, and σ-opioid receptors, Naltrexone has greater oral efficacy and longer duration of action than naloxone. Naltrexone treatment caused a doubling in the density of [3H]DAMGO binding sites in both whole brain membranes and the 7315c cell membranes. Naltrexone treatment may have slightly diminished the affinity of mu opioid receptors for [3H]DAMGO (by 1.5- to 2-fold), but the precision of the assay was inadequate to determine whether this difference was significant. Naltrexone treatment also had no effect on the potency or efficacy of guanosine 5'-O-(3-thiotriphosphate) in diminishing [3H]DAMGO binding to either whole brain or 7315c cell membranes. Naltrexone which has no SP receptor antagonistic action, not only indirectly acts on SP-ergic neurons but also causes a change in the apparent affinity of NK-1 receptor (as reflected by changes in IC50 values) in the striatum. Cellular inositol-1,4,5-trisphosphate [Ins(1,4,5)P3], quantified by a highly sensitive and selective radioreceptor mass assay, was increased in the striatum by 28% relative to control levels.

Tiihonen J, et al. Naltrexone implant for the treatment of polydrug dependence: a randomized controlled trial. Am J Psychiatry. 2012 May;169(5):531-6. Sun L, Wang T, Gao L, Quan D, Feng D.Multivesicular liposomes for sustained release of naltrexone hydrochloride: design, characterization and in vitro/in vivo evaluation.Pharm Dev Technol. 2012 Jul 3. Zukin RS, Sugarman JR, Fitz-Syage ML et al. Naltrexone-induced opiate receptor supersensitivity. Brain Res. 1982 Aug 12;245(2):285-92. Naltrexone hydrochloride Naltrexone