Zakoprid

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Zakoprid
(IUPAC) ime
4-amino-5-hloro-2-metoksi-N-(hinuklidin-3-il)benzamid
Klinički podaci
Identifikatori
CAS broj 90182-92-6
ATC kod nije dodeljen
PubChem[1][2] 108182
UNII 9GN3OT4156 YesY
ChEMBL[3] CHEMBL18041 YesY
Hemijski podaci
Formula C15H20ClN3O2 
Mol. masa 309,791 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status

Zakoprid je potencijalni antagonist 5HT3 receptora[4] i agonist 5HT4 receptora.[5]R enantiomer aktivna forma.[6] On ispoljava anksiolitska[7] i nootropna svojstva na životinjskim modelima.[8] On je isto ima antiemetske[9] i prorespiratorne osobine. On redukuje aprenju u snu[10] i poništava opioidom indukovanu respiratornu depresiju u životinjskim studijama.[11]

Reference[uredi - уреди | uredi izvor]

  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. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.  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. 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. PMID 21948594. doi:10.1093/nar/gkr777.  edit
  4. Smith, WW; Sancilio, LF; Owera-Atepo, JB; Naylor, RJ; Lambert, L (1988). "Zacopride, a potent 5-HT3 antagonist". The Journal of pharmacy and pharmacology 40 (4): 301–2. PMID 2900319. doi:10.1111/j.2042-7158.1988.tb05253.x. 
  5. Lefebvre, H; Contesse, V; Delarue, C; Soubrane, C; Legrand, A; Kuhn, JM; Wolf, LM; Vaudry, H (1993). "Effect of the serotonin-4 receptor agonist zacopride on aldosterone secretion from the human adrenal cortex: in vivo and in vitro studies". The Journal of Clinical Endocrinology and Metabolism 77 (6): 1662–6. PMID 8263156. doi:10.1210/jc.77.6.1662. 
  6. Young, R; Johnson, DN (1991). "Anxiolytic-like activity of R(+)- and S(-)-zacopride in mice". European Journal of Pharmacology 201 (2–3): 151–5. PMID 1686755. doi:10.1016/0014-2999(91)90338-Q. 
  7. Costall, B; Domeney, AM; Gerrard, PA; Kelly, ME; Naylor, RJ (1988). "Zacopride: anxiolytic profile in rodent and primate models of anxiety". The Journal of pharmacy and pharmacology 40 (4): 302–5. PMID 2900320. doi:10.1111/j.2042-7158.1988.tb05254.x. 
  8. Fontana, DJ; Daniels, SE; Eglen, RM; Wong, EH (1996). "Stereoselective effects of (R)- and (S)-zacopride on cognitive performance in a spatial navigation task in rats". Neuropharmacology 35 (3): 321–7. PMID 8783207. doi:10.1016/0028-3908(96)00191-8. 
  9. Yamakuni, H; Nakayama, H; Matsui, S; Imazumi, K; Matsuo, M; Mutoh, S (2006). "Inhibitory effect of zacopride on Cisplatin-induced delayed emesis in ferrets". Journal of pharmacological sciences 101 (1): 99–102. PMID 16651699. doi:10.1254/jphs.SCJ05007X. 
  10. Carley, DW; Depoortere, H; Radulovacki, M (2001). "R-zacopride, a 5-HT3 antagonist/5-HT4 agonist, reduces sleep apneas in rats". Pharmacology, Biochemistry, and Behavior 69 (1–2): 283–9. PMID 11420096. doi:10.1016/S0091-3057(01)00535-4. 
  11. Meyer, LC; Fuller, A; Mitchell, D (2006). "Zacopride and 8-OH-DPAT reverse opioid-induced respiratory depression and hypoxia but not catatonic immobilization in goats". American journal of physiology. Regulatory, integrative and comparative physiology 290 (2): R405–13. PMID 16166206. doi:10.1152/ajpregu.00440.2005. 

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