Naltrexone hydrochloride Inhibitor CAS No. 16676-29-2 - Naltrexone hydrochloride Supplier

Product Name	Naltrexone hydrochloride
Synonyms	Revia, Depade, Vivitrol, Trexan
CAS No.	16676-29-2
Molecular Weight	377.86
Formula	C₂₀H₂₄ClNO₄
Chemical Structure

Biological activities

Naltrexone hydrochloride is a hydrochloride salt of naltrexone. Naltrexone is a µ- and κ-opioid receptors antagonist. The IC50 of naltrexone is 4.1 nM against µ-opioid receptor.^[1] Naltrexone inhibits µ-opioid receptor with a Ki of 0.27 nM in the electrically-stimulated guinea pig ileum.^[2] Naltrexone reveals 2-fold higher affinity and potency than 6β-naltrexol for the µ-opioid receptor binding site and for µ-opioid receptor agonist-stimulated [³⁵S]GTP_{γS binding, respectively.^[3] Naltrexone non-competitively inhibits α7 neuronal nicotinic receptors (nAChRs) with an IC50 of∼25 µM. Naltrexone also prevents activation of α4β2 nAChRs in hippocampal neurons. Naltrexone at the doses of 0.3 and 30 µM blocks the increases in number of neurons expressing functional non-α7 nAChRs. ^[4] Pretreatment with 10 mg/kg naltrexone attenuates the antagonist effects of β-FNA in male rats.^[5] Naltrexone dose-dependently blocks morphine's immunomodulatory effects.^[6]}

Protocols

In vivo: Naltrexone is dissolved in saline at doses of 0.1, 1.0 or 10.0 mg/kg.^[6]

References

[1] Le Bourdonnec B, et al. Elucidation of the bioactive conformation of the N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine class of mu-opioid receptor antagonists. J Med Chem. 2006, 49(25): 7278-7289. 閵嗏偓閵嗏偓 [2] Porter SJ, et al. In vivo and in vitro potency studies of 6β-naltrexol, the major human metabolite of naltrexone. Addict Biol. 2002, 7(2): 219-225. 閵嗏偓閵嗏偓 [3] Ko MC, et al. Differential in vivo potencies of naltrexone and 6β-naltrexol in the monkey. J Pharmacol Exp Ther. 2006, 316(2): 772-779. 閵嗏偓閵嗏偓 [4] Almeida LE, et al. The opioid antagonist naltrexone inhibits activity and alters expression of α7 and α4β2 nicotinic receptors in hippocampal neurons: implications for smoking cessation programs. Neuropharmacology. 2000, 39(13): 2740-2755. 閵嗏偓閵嗏偓 [5] Paronis CA, et al. Naltrexone in vivo protects mu receptors from inactivation by beta-funaltrexamine, but not kappa receptors from inactivation by nor-binaltorphimine. Pharmacol Biochem Behav. 1993, 46(4): 813-817. 閵嗏偓閵嗏偓 [6] Lysle DT, et al. Morphine-induced alterations of immune status: dose dependency, compartment specificity and antagonism by naltrexone. J Pharmacol Exp Ther. 1993, 265(3): 1071-1078. 閵嗏偓閵嗏偓

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