|Systematic (IUPAC) name|
|Mol. mass||308.3329 g/mol|
In studies it proved to be a potent and highly selective dopamine reuptake inhibitor (DRI) in rat brain preparations. A study found a moderately long half-life of approximately 12 hours and a dopaminergic potency approximately 50 fold that of methylphenidate in rat brain preparations. Despite lack of direct serotonin activity, rats treated with subchronic doses of amfonelic acid display subsequent decreases in 5HT and 5HIAA. Amfonelic acid displays no activity in the norepinephrine system.
Amfonelic acid has been shown to be neuroprotective against methamphetamine damage to dopamine neurons. It also increases the effects of the antipsychotic drugs haloperidol, trifluoperazine and spiperone.
Amfonelic acid is not a controlled substance in the United States, and thus is legal to possess.
- US patent 3590036, "Naphthyridine-3-carboxylic Acids, Their Derivatives and Preparation Thereof"
- Fuller, R. W.; Perry, K. W.; Bymaster, F. P.; Wong, D. T. (1978). "Comparative effects of pemoline, amfonelic acid and amphetamine on dopamine uptake and release in vitro and on brain 3,4-dihydroxyphenylacetic acid concentration in spiperone-treated rats.". Journal of Pharmacy and Pharmacology 30 (3): 197–198.
- McMillen, B. A.; Shore, P. A. (1978). "Amfonelic acid, a non-amphetamine stimulant, has marked effects on brain dopamine metabolism but not noradrenaline metabolism: Association with differences in neuronal storage systems". Journal of Pharmacy and Pharmacology 30 (7): 464–466.
- Izenwasser, S.; Werling, L. L.; Cox, B. M. (1990). "Comparison of the effects of cocaine and other inhibitors of dopamine uptake in rat striatum, nucleus accumbens, olfactory tubercle, and medial prefrontal cortex". Brain Research 520 (1–2): 303–309.
- McMillen, BA; Scott, SM; Williams, HL (1991). "Effects of subchronic amphetamine or amfonelic acid on rat brain dopaminergic and serotonergic function". Journal of neural transmission. General section 83 (1–2): 55–66.
- Agmo, A; Belzung, C; Rodríguez, C (1997). "A rat model of distractibility: Effects of drugs modifying dopaminergic, noradrenergic and GABAergic neurotransmission". Journal of neural transmission (Vienna, Austria : 1996) 104 (1): 11–29.
- Aceto, MD; Rosecrans, JA; Young, R; Glennon, RA (1984). "Similarity between (+)-amphetamine and amfonelic acid". Pharmacology, Biochemistry, and Behavior 20 (4): 635–7.
- Pu, C; Fisher, JE; Cappon, GD; Vorhees, CV (1994). "The effects of amfonelic acid, a dopamine uptake inhibitor, on methamphetamine-induced dopaminergic terminal degeneration and astrocytic response in rat striatum". Brain Research 649 (1–2): 217–24.
- Waldmeier, PC; Huber, H; Heinrich, M; Stoecklin, K (1985). "Discrimination of neuroleptics by means of their interaction with amfonelic acid: An attempt to characterize the test". Biochemical pharmacology 34 (1): 39–44.
- Porrino, LJ; Goodman, NL; Sharpe, LG (1988). "Intravenous self-administration of the indirect dopaminergic agonist amfonelic acid by rats". Pharmacology, Biochemistry, and Behavior 31 (3): 623–6.
- KEGG PATHWAY DATABASE : AMFONELIC ACID