Zakoprid
Zakoprid je potencijalni antagonist 5HT3 receptora[1] i agonist 5HT4 receptora.[2]R enantiomer aktivna forma.[3] On ispoljava anksiolitska[4] i nootropna svojstva na životinjskim modelima.[5] On je isto ima antiemetske[6] i prorespiratorne osobine. On redukuje aprenju u snu[7] i poništava opioidom indukovanu respiratornu depresiju u životinjskim studijama.[8]
 | |
| IUPAC ime | |
|---|---|
4-amino-5-hloro-2-metoksi-N-(hinuklidin-3-il)benzamid | |
| Identifikatori | |
| CAS broj | 90182-92-6  |
| ATC kod | none |
| PubChem | CID 108182 |
| IUPHAR/BPS | 245 |
| UNII | 9GN3OT4156 |
| ChEMBL | CHEMBL18041 |
| Hemijski podaci | |
| Formula | C15H20ClN3O2 |
| Molarna masa | 309,791 g/mol |
| |
Reference
уреди- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
