product name Naltrexone HCl
Description: Naltrexone HCl is a potent opioid receptor antagonist used mainly in the management of alcohol dependence and opioid dependence. Naltrexone is a drug that reverses the effects of opioids and should not be confused with naloxone or nalorphine, which are used in emergency cases of opioid overdose. Opioid receptor is a group of G protein-coupled receptors with opioids as ligands (e.g. proenkephalin, prodynorphin, pronociceptin etc, functioning in regulating pain perception, hormonal secretion and affecting temperature control etc.
References: Psychopharmacology (Berl). 1998 Sep;139(1-2):53-61; Eur J Pharmacol. 1999 Jun 25;374(3):321-7.
377.86
Formula
C20H23NO4.HCl
CAS No.
16676-29-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 14 mg/mL (37.1mM)
Water: 14 mg/mL (37.1mM)
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: Naltrexone (0.32 mg/kg) reduces ethanol-reinforced responding at the concentration that maintained the most responding (1% or 2%) in rhesus monkeys. Naltrexone (0.1 mg/kg) reduces ethanol-reinforced responding, both at a low ethanol concentration (0.25%) that produced little ethanol intake (g/kg), and at a higher concentration (4%) with an appreciable intake. Naltrexone (1-3 mg/kg) potently and dose-dependently inhibits reinstatement of ethanol-seeking produced by non-contingent deliveries of the liquid dipper filled with 8% ethanol. Naltrexone elicits optimal enhancement of morphines antinociceptive potency in mice when co-administered (i.p.) at about 100 ng/kg together with morphine (3 mg/kg). Naltrexone (10 ng/kg i.p.) augments the antinociception produced by an acute submaximal dose of intrathecal (5 mg) or systemic (7.5 mg/kg i.p.) morphine in the tail-flick test in rats. Naltrexone combined with Morphine inhibits the decline in morphine antinociception and prevented the loss of morphine potency in rats. Naltrexone significantly suppresses ethanol self-administration and prevents ethanol-induced increases in dialysate dopamine levels. Naltrexone completely prevents the reduction in anogenital distance in prenatally stressed (PS) males and restores the growth rate of both sexes. Naltrexone also decreases the anxiety of PS rats in the plus-maze, increases the opioid component of exploration to control levels, but increases anxiety in control males Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | In adult male Sprague-Dawley rats, ultra-low doses of naltrexone (16.7, 20.0, and 25.0 ng/kg) with morphine (1mg/kg) extended the duration of the morphine-induced conditioned place preference. In male Wistar rats, naltrexone significantly inhibited ethanol self-adminnistration and prevented ethanol-activated increases in dialysate dopamine amount. Subchronic treatment with naltrexone caused progressive decrease of ethanol self-administration. Single doses of naltrexone increased extinction and attenuated cue-induced reinstatement of ethanol-reinforced behavior. In rhesus monkeys, naltrexone lowered behavior kept non-selectively by either ethanol or sucrose. |
| Animal model | Male Sprague-Dawley rats, |
| Formulation & Dosage | 16.7, 20.0, and 25.0 ng/kg |
| References | Psychopharmacology (Berl). 1998 Sep;139(1-2):53-61; Eur J Pharmacol. 1999 Jun 25;374(3):321-7. |
