Disease relevance of Amfonelic acid

• Reuptake blockers for norepinephrine (desmethylimipramine [17%], tomoxepine [31%], but not amfonelic acid [82%]) decreased the frequency of duodenal ulcers [1].
• Amfonelic acid alone produced hyperalgesia and completely antagonized the analgesic effect of morphine [2].

Psychiatry related information on Amfonelic acid

• The stimulation of locomotor activity by amfonelic acid in C57B1/6 mice was more sensitive to the blocking effect of ethanol than stimulation induced by d-amphetamine [3].
• In a test for social and exploratory behaviors it was found that amfonelic acid, in a dose of 0.5 mg/kg, augmented sniffing and rearing without affecting nonsexual interaction with a receptive female [4].
• Amfonelic acid, a compound that enhances dopaminergic tone by a complex mechanism, increased aspects of both appetitive and consummatory behaviors [5].

High impact information on Amfonelic acid

• However, analysis of DA reuptake kinetics obtained in the absence and presence of DAT blockade (by cocaine and amfonelic acid) revealed only minor differences in DAT functionality [6].
• Uptake of MPP+ and dopamine into both rat and human synaptosomes was inhibited by cocaine and amfonelic acid, with the latter being five to 10 times more potent than the former [7].
• Pretreatment with amfonelic acid, a potent DA uptake inhibitor, significantly reduced the effect of DHT on striatal and nigral TH activity and striatal DA concentration without affecting the DHT-induced decrease in striatal TPH activity [8].
• There did appear to be some degree of heterogeneity of binding sites for [3H]GBR 12935 in each of these regions of the brain, as both amfonelic acid and mazindol were best fitted by two-site models [9].
• However, though amfonelic acid acted as a strong releaser of DA in Swiss-Webster, CD-1, DBA-2 and BALB/c mice, in these strains it failed to reduce the effect of ethanol [3].

Anatomical context of Amfonelic acid

• The effects of amfonelic acid on the neuroleptic-induced changes in extracellular DOPAC were greater in the striatum than the nucleus accumbens [10].
• In rats treated systemically with either amphetamine, amfonelic acid or apomorphine, large numbers of cells displaying Fos-like immunoreactivity (FLI) could be seen in the lateral zone of the lateral habenula [11].
• The present study compares the effects of d-amphetamine (d-AMP) and the potent non-amphetamine CNS stimulant, amfonelic acid (AFA), on the firing rate of single midbrain dopaminergic (DA) neurons and on neostriatal DA metabolism (dihydroxyphenylacetic acid--DOPAC) [12].

Associations of Amfonelic acid with other chemical compounds

• Compounds known to inhibit [3H]dopamine uptake in vitro, such as nomifensine, 4-hydroxy-nomifensine, mazindol, amfonelic acid and benztropine, were the most potent competitors of nomifensine binding [13].
• Tyramine and amfonelic acid in low concentrations enhanced the spontaneous outflow of radioactivity and, similarly to amphetamine, inhibited the electrically evoked release of [3H]dopamine [14].
• In addition, the administration of the specific dopamine uptake blocker, amfonelic acid, significantly attenuated the changes in the serotonin synthesizing enzyme, tryptophan hydroxylase, resulting from multiple high doses of methamphetamine [15].
• This study compares the effects of the nonamphetamine stimulant amfonelic acid on the increase in extracellular 3,4-dihydroxyphenylacetic acid (DOPAC) induced by haloperidol and clozapine in the nucleus accumbens and the striatum of anaesthetized rats [10].
• Coadministration of the dopamine uptake inhibitor, amfonelic acid, selectively prevented the methamphetamine-induced decrease in tyrosine hydroxylase activity while not altering the depression of tryptophan hydroxylase activity [16].

Gene context of Amfonelic acid

• In pimozide-pretreated mice, amfonelic acid failed to reduce the ethanol-induced hypnosis [3].
• The results also indicate that neurotensin in the presence of amfonelic acid has a profile similar to the atypical neuroleptics [17].
• The ability of amfonelic acid to distinguish between the actions of clozapine and haloperidol on nigrostriatal and mesocorticolimbic DA neurons does not appear to be related to differences in the effects of the drugs on DA autoreceptors or 5-HT2 receptors [18].

Analytical, diagnostic and therapeutic context of Amfonelic acid

• Intravenous self-administration of the indirect dopaminergic agonist amfonelic acid by rats [19].

References