Description
Selective and potentδ-opioid receptor antagonist (Kivalues are 0.013, 19 and 152 nM forδ,μandκreceptors respectively). Displays selectivity for theδ2subtypein vivo.
Uses
Naltriben mesylate is a potent δ2-opioid receptor antagonist and a TRPM7 activator. Naltriben mesylate shows Ki values of 0.013 nM, 19 nM and 152 nM for δ, μ and κ receptors, respectively. Naltriben mesylate enhances glioblastoma cell migration and invasion. Naltriben mesylate can be used in research into neurological diseases and cancer[1][2].
in vivo
The hypothermia caused by SNC-80 (35 mg/kg, im) is blocked by a delta2 antagonist, Naltriben (2.5 mg/kg; sc; Sprague-Dawley rats weighing 100-125 g)[2].
References
[1] Krishnan-Sarin S, Portoghese PS, Li TK, Froehlich JC. The delta 2-opioid receptor antagonist naltriben selectively attenuates alcohol intake in rats bred for alcohol preference. Pharmacol Biochem Behav. 1995;52(1):153-159. DOI:
10.1016/0091-3057(95)00080-g[2] Rawls SM, et al. Brain delta2 opioid receptors mediate SNC-80-evoked hypothermia in rats. Brain Res. 2005;1049(1):61-69. DOI:
10.1016/j.brainres.2005.04.074
