Alaproklat

Alaproklat
(IUPAC) ime
1-(4-chlorophenyl)-2-methylpropan-2-yl 2-aminopropanoate
Klinički podaci
Identifikatori
CAS broj 60719-82-6
60719-83-7 (hidrohlorid)
ATC kod N06AB07
PubChem[1][2] 2081
ChemSpider[3] 1997
KEGG[4] D02787 DaY
ChEMBL[5] CHEMBL36591 DaY
Hemijski podaci
Formula C13H18ClNO2 
Mol. masa 255.740 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status nije kontrolisan
Način primene Oralno

Alaproklat (GEA-654) je psihoaktivni lek i istraživačka hemikalija koja je bila u razvoju kao antidepresiv[6] od strane švedske farmaceutske kompanije Astra AB (sadašnja AstraZeneca) tokom 1970-ih. On deluje kao selektivni inhibitor preuzimanja serotonina (SSRI)[7], i zajedno sa zimelidinom i indalpinom, je bio jedan od prvih lekova iz te klase. Njegov razvoj je prekinut kao posledica hepatotoksičnosti u studijama na glodarima. Utvrđeno je da deluje kao nekompetitivni NMDA antagonist, ali da nije selektivan poput fenciklidina.[8][9]

Literatura

  1. ↑ 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.  edit
  2. ↑ 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. 
  3. ↑ 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.  edit
  4. ↑ Joanne Wixon, Douglas Kell (2000). „Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG”. Yeast 17 (1): 48–55. DOI:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H. 
  5. ↑ Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594.  edit
  6. ↑ Danysz W, Plaznik A, Kostowski W, Malatynska E, Järbe TU, Hiltunen AJ, Archer T (January 1988). „Comparison of desipramine, amitriptyline, zimeldine and alaproclate in six animal models used to investigate antidepressant drugs”. Pharmacology & Toxicology 62 (1): 42–50. PMID 2965810. 
  7. ↑ Jäkälä P, Sirviö J, Riekkinen P, Valjakka A, Riekkinen P (1992). „The effects of alaproclate and p-chlorophenylalanine on cued navigation performance in rats”. Journal of Neural Transmission. Parkinson's Disease and Dementia Section 4 (1): 43–52. PMID 1531758. 
  8. ↑ A Wilkinson, M Courtney, A Westlind-Danielsson, G Hallnemo and K E Akerman (December 1994). „Alaproclate acts as a potent, reversible and noncompetitive antagonist of the NMDA receptor coupled ion flow”. JPET 271 (3): 1314–1319. 
  9. ↑ K L Nicholson and R L Balster (2003-04-23). „Evaluation of the phencyclidine-like discriminative stimulus effects of novel NMDA channel blockers in rats”. Psychopharmacology.