Naftilizopropilamin
Naftilizopropilamin (PAL-287) je eksperimentalni lek koje se istražuje kao potencijalni tretmant za alkoholnu i stimulansnu adikciju.[4]
| |||
| (IUPAC) ime | |||
|---|---|---|---|
| (±)-1-(2-naftil)propan-2-amin | |||
| Klinički podaci | |||
| Identifikatori | |||
| CAS broj | 18085-03-5 | ||
| ATC kod | nije dodeljen | ||
| PubChem[1][2] | 10219723 | ||
| ChemSpider[3] | 8395215 | ||
| Hemijski podaci | |||
| Formula | C13H15N | ||
| Mol. masa | 185,27 g/mol | ||
| SMILES | eMolekuli & PubHem | ||
| |||
| Sinonimi | 1-(2-naftil)-2-aminopropan; alfa-metilnaptiletilamin | ||
| Farmakoinformacioni podaci | |||
| Trudnoća | ? | ||
| Pravni status | Nije kontrolisan | ||
| Način primene | Oralno | ||
Naftilizopropilamin deluje kao agens otpuštanja serotonina, norepinefrina, i dopamina koji nije neurotoksičan[5], sa EC50 vrednostima od 3,4 nM, 11,1 nM, i 12,6 nM, respektivno.[6] 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),[4] 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.[4]
U životinjskim studijama, je pokazano da naftilizopropilamin redukuje kokainsku samoadministraciju, mada ima relativno slam stimulatorni efekat kad se samostalno dozira.[5][7][8][9]
Reference
uredi- ↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519.
- ↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
- ↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846.
- ↑ 4,0 4,1 4,2 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. DOI:10.1208/aapsj0901001. PMC 2751297. PMID 17408232.
- ↑ 5,0 5,1 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. DOI:10.1124/jpet.104.082503. PMID 15761112.
- ↑ 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. DOI:10.1124/jpet.104.080101. PMID 15677348.
- ↑ 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. DOI:10.1016/S0091-3057(84)80071-4. PMID 6522418.
- ↑ 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. DOI:10.1124/jpet.106.107383. PMID 17071819.
