Disease relevance of Etonitazine

• As the drug concentration was increased, the number of liquid deliveries decreased, and etonitazene intake (microgram/kg body weight) increased [1].
• The 75% weight group showed stereotypy, self-mutilation and large variability in daily etonitazene intake [2].
• Sensitivity to etonitazene-induced respiratory depression, stimulation of locomotor activity and analgesia were unrelated to drug intake during self-administration sessions across these four inbred strains.(ABSTRACT TRUNCATED AT 250 WORDS)[3]
• Intraventricular morphine infusions resulted in explosive motor behavior whereas etonitazene produced extreme muscular rigidity [4].

Psychiatry related information on Etonitazine

• Another group of rats with implanted jugular catheters self-administered etonitazene (10 micrograms per kilogram) intravenously on a continuous reinforcement schedule, and the number of infusions increased significantly on days when they were deprived of food [5].
• 1-(BETA-Kiethylaminoethyl)-2-(p-ethoxybenzyl)-5-nitrobenzimidazole (u, etonitazene) is a potent analgesic that has value in drug addiction studies [6].
• Etonitazene as a reinforcer for rats: increased etonitazene-reinforced behavior due to food deprivation [7].
• A wide range of etonitazene doses (5-80 micrograms/kg) and saline were tested under food satiation and food deprivation conditions [8].
• Concurrent etonitazene and water intake in rats: role of taste, olfaction, and auditory stimuli [9].

High impact information on Etonitazine

• Moreover, we have recently demonstrated that the high-efficacy agonist etonitazene promotes rapid endocytosis of micro-opioid receptors, whereas the agonist morphine and the low-efficacy agonist buprenorphine fail to promote detectable receptor endocytosis in micro-opioid receptor expressing HEK293 cells [10].
• The 5'D-II activity was significantly enhanced 30 min after administration of etonitazene in the frontal cortex, amygdala and limbic forebrain, and after administration of ethanol in the amygdala alone [11].
• The apparent in vivo dissociation constant (KA) and relative efficacy values for alfentanil, etonitazene, morphine, and nalbuphine were determined by comparing the effects of these agonists in the presence of buprenorphine with the effects of these agonists alone in the rhesus monkey tail-withdrawal procedure [12].
• To assess the acquisition and maintenance of opioid reinforced behavior, oral self-administration of the potent benzimidazole opioid, etonitazene, was determined using an operant fixed-ratio schedule of reinforcement (FR 8) [3].
• C-CAM produced dose-dependent rightward and slight downward shifts of the etonitazene dose-effect curve [13].

Biological context of Etonitazine

• These findings demonstrate genetic differences in opioid reinforcement of operant behavior and indicate that genotype can be an important determinant of whether etonitazene serves as a reinforcer [14].

Anatomical context of Etonitazine

• Effects of etonitazene consumption and abstinence on the signal transmission of mu-opioid receptors in brain membranes of rats [15].

Associations of Etonitazine with other chemical compounds

• These results indicate that heroin, 6-acetylmorphine, fentanyl and etonitazine all can produce analgesia through a novel mu analgesic system which is similar to that activated by morphine-6 beta-glucuronide [16].
• However, diltiazem failed to alter the analgesic potencies of the mu-opioid receptor agonists, fentanyl, etonitazene, nalbuphine, the kappa-opioid receptor agonist, U-50,488 [(trans)-3, 4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)-cyclohexyl]benzeneacetamide ], or the non-opioid, clonidine [17].

Gene context of Etonitazine

• Antisense mapping of the mu opioid receptor MOR-1 reveals that oligodeoxynucleotide probes against exon 2, which are inactive against morphine analgesia, block morphine-6 beta-glucuronide, heroin, fentanyl and etonitazine analgesia [16].
• Furthermore, naloxone, but not etonitazene, resulted in a significant increase in the Bmax of TCP binding to the PCP receptor [18].
• Two groups of naive, male, albino rats derived from different genetic strains (Sprague-Dawley and Wistar) were given a 5 micrograms/ml etonitazene solution as their only available liquid [19].

Analytical, diagnostic and therapeutic context of Etonitazine

• Together with data previously obtained in drug discrimination and analgesia assays, results of the present study demonstrating homogeneous pA2 values for quadazocine with alfentanil, etonitazene, EKC and Mr2033 strongly suggest that the latter two compounds decrease respiratory function in rhesus monkeys by acting on mu receptors [20].
• Reinforcing effects of contingently administered subcutaneous injections of etonitazene in rats [21].
• In all strains, only the paired treatment condition demonstrated tolerance to the analgesic effects of etonitazene compared to the control groups [22].

References