Zakoprid

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	108182
UNII	9GN3OT4156
ChEMBL	CHEMBL18041
Hemijski podaci
Formula	C15H20ClN3O2
Mol. masa	309,791 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C15H20ClN3O2/c1-21-14-7-12(17)11(16)6-10(14)15(20)18-13-8-19-4-2-9(13)3-5-19/h6-7,9,13H,2-5,8,17H2,1H3,(H,18,20) ; Key: FEROPKNOYKURCJ-UHFFFAOYSA-N
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

↑ 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
↑ 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.
↑ 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
↑ 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. DOI:10.1111/j.2042-7158.1988.tb05253.x. PMID 2900319.
↑ 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. DOI:10.1210/jc.77.6.1662. PMID 8263156.
↑ Young, R; Johnson, DN (1991). „Anxiolytic-like activity of R(+)- and S(-)-zacopride in mice”. European Journal of Pharmacology 201 (2–3): 151–5. DOI:10.1016/0014-2999(91)90338-Q. PMID 1686755.
↑ 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. DOI:10.1111/j.2042-7158.1988.tb05254.x. PMID 2900320.
↑ 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. DOI:10.1016/0028-3908(96)00191-8. PMID 8783207.
↑ 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. DOI:10.1254/jphs.SCJ05007X. PMID 16651699.
↑ 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. DOI:10.1016/S0091-3057(01)00535-4. PMID 11420096.
↑ 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. DOI:10.1152/ajpregu.00440.2005. PMID 16166206.

Vanjske veze

	Portal Medicina
	Portal Hemija

[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] 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

[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. DOI:10.1111/j.2042-7158.1988.tb05253.x. PMID 2900319.

[Lefebvre1993-5] 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. DOI:10.1210/jc.77.6.1662. PMID 8263156.

[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. DOI:10.1016/0014-2999(91)90338-Q. PMID 1686755.

[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. DOI:10.1111/j.2042-7158.1988.tb05254.x. PMID 2900320.

[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. DOI:10.1016/0028-3908(96)00191-8. PMID 8783207.

[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. DOI:10.1254/jphs.SCJ05007X. PMID 16651699.

[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. DOI:10.1016/S0091-3057(01)00535-4. PMID 11420096.

[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. DOI:10.1152/ajpregu.00440.2005. PMID 16166206.

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