Naftilizopropilamin
Naftilizopropilamin (PAL-287) je eksperimentalni lek koje se istražuje kao potencijalni tretmant za alkoholnu i stimulansnu adikciju.[1]
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| IUPAC ime | |
|---|---|
(±)-1-(2-naftil)propan-2-amin | |
| Klinički podaci | |
| Kategorija trudnoće |
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| Način primene | Oralno |
| Pravni status | |
| Pravni status |
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| Identifikatori | |
| CAS broj | 18085-03-5  |
| ATC kod | none |
| PubChem | CID 10219723 |
| ChemSpider | 8395215 |
| Sinonimi | 1-(2-naftil)-2-aminopropan; alfa-metilnaptiletilamin |
| Hemijski podaci | |
| Formula | C13H15N |
| Molarna masa | 185,27 g/mol |
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Naftilizopropilamin deluje kao agens otpuštanja serotonina, norepinefrina, i dopamina koji nije neurotoksičan[2], sa EC50 vrednostima od 3,4 nM, 11,1 nM, i 12,6 nM, respektivno.[3] On takođe ima visok afinitet za 5-HT2A, 5-HT2B, i 5-HT2C receptore (EC50 vrednosti = 466 nM, 40 nM, i 2.3 nM, respektivno),[1] i deluje kao pun agonist na 5-HT2B i kao parcijalni agonist na 5-HT2C, dok je njegov afinitet za 5-HT2A verovatno suviše nizak da bi bio značajan.[1]
U životinjskim studijama, je pokazano da naftilizopropilamin redukuje kokainsku samoadministraciju, mada ima relativno slam stimulatorni efekat kad se samostalno dozira.[2][4][5][6]
Reference
уреди- ^ а б в Rothman, Richard B.; Blough, Bruce E.; Baumann, Michael H. (2007). „Dual dopamine/serotonin releasers as potential medications for stimulante and alcohol addictions”. The AAPS Journal. 9 (1): E1—E10. PMC 2751297
. PMID 17408232. doi:10.1208/aapsj0901001.
- ^ а б Rothman, R. B.; Blough, BE; Woolverton, WL; Anderson, KG; Negus, SS; Mello, NK; Roth, BL; Baumann, MH (2005). „Development of a Rationally Designed, Low Abuse Potential, Biogenic Amine Releaser That Suppresses Cocaine Self-Administration”. Journal of Pharmacology and Experimental Therapeutics. 313 (3): 1361—1369. PMID 15761112. doi:10.1124/jpet.104.082503.
- ^ Wee, S.; Anderson, KG; Baumann, MH; Rothman, RB; Blough, BE; Woolverton, WL (2004). „Relationship between the Serotonergic Activity and Reinforcing Effects of a Series of Amphetamine Analogs”. Journal of Pharmacology and Experimental Therapeutics. 313 (2): 848—854. PMID 15677348. doi:10.1124/jpet.104.080101.
- ^ Mehes, G (1952). „On the pharmacological effects of 1-(alpha-naphthyl)-, and 1-(beta-naphthyl)-2-aminopropane; a contribution on the problem of chemical structure and effect”. Acta physiologica Hungarica. 3 (1): 137—51. PMID 13050439.
- ^ Glennon, RA; Young, R; Hauck, AE; McKenney, JD (1984). „Structure-activity studies on amphetamine analogs using drug discrimination methodology”. Pharmacology, Biochemistry, and Behavior. 21 (6): 895—901. PMID 6522418. doi:10.1016/S0091-3057(84)80071-4.
- ^ Negus, S. S.; Mello, N. K.; Blough, B. E.; Baumann, M. H.; Rothman, R. B. (2006). „Monoamine Releasers with Varying Selectivity for Dopamine/Norepinephrine versus Serotonin Release as Candidate "Agonist" Medications for Cocaine Dependence: Studies in Assays of Cocaine Discrimination and Cocaine Self-Administration in Rhesus Monkeys”. Journal of Pharmacology and Experimental Therapeutics. 320 (2): 627—636. PMID 17071819. doi:10.1124/jpet.106.107383.
