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Chemical Compound Review

Zacoprida     4-amino-N-(1- azabicyclo[2.2.2]oct-8-yl)- 5...

Synonyms: Zacopride, Zacopridum, iodozacopride, CHEMBL18041, SureCN16003, ...
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Disease relevance of Zacopride


Psychiatry related information on Zacopride


High impact information on Zacopride


Chemical compound and disease context of Zacopride


Biological context of Zacopride


Anatomical context of Zacopride

  • Zacopride and ICS 205-930 showed similar affinity (-log kB approximately 8.0), whereas GR38032F showed lower affinity (-log ka approximately 7.0) at 5-HT3 receptors in the guinea pig ileum [3].
  • 2. Racemic zacopride, and both of the enantiomers, displayed potent 5-HT3 receptor antagonist activity in the isolated vagus nerve and in the von Bezold-Jarisch model [20].
  • Zacopride (intragastric, 0.3 mg/kg) or a placebo was given blindly and randomly in the basal state and 15 min before a whole-body 800 cGy 60Co gamma-radiation dose (except for the legs which were partially protected to permit survival of some bone marrow) [21].
  • Substitution of the chlorine atom by a radio-iodine in position 5 in the zacopride molecule yielded [125I]iodo-zacopride that bound with high affinity (Kd = 4.3 nM) to 5-HT3 receptors in the rat central nervous system [22].
  • In well-washed striatal membranes, neither zacopride nor ICS 205-930 (10(-9)-10(-5) M) inhibited [3H]2 beta-carbomethoxy-3 beta-(4-fluorophenyl)tropane ([3H]WIN 35,428) (0.3 nM) binding [23].

Associations of Zacopride with other chemical compounds


Gene context of Zacopride

  • In addition, the stimulation of PI turnover by 2-Me-5-HT was antagonized stereospecifically by the 5-HT3 receptor blocker zacopride [28].
  • 5HT1c receptor antagonists (mianserin and cyproheptadine), 5-HT3 receptor antagonist (zacopride) and 5-HT4 receptor antagonist (ICS 205-930) increased the latency of audiogenic seizures and decreased the severity of convulsions in young (20-27 days old) DBA/2 mice [29].
  • In addition, the 5-HT3 antagonist zacopride failed to attenuate aggression or produce debilitation at any of the doses tested; however, the 5-HT2 antagonist ritanserin inhibited aggressive behavior at a high dose which was not debilitating [30].
  • The effect of both agonists was reversed by prior local microinjection of the 5-HT3 receptor antagonists zacopride (100 pmol) and ondansetron (100 pmol), but not by that of the 5-HT2 receptor antagonist ketanserin (10 pmol) or the mixed 5-HT1/5-HT2 receptor antagonist methysergide (100 pmol) [31].
  • The racemic 5-HT3 receptor antagonist, zacopride (10-100 micrograms kg-1, i.m.) evoked an emetic response in ferrets [32].

Analytical, diagnostic and therapeutic context of Zacopride

  • Similarly, co-administration of either 25-100 micro M LY-278-584 or 10-100 micro M zacopride with 200 mg% EtOH completely blocked EtOH-maintained intracranial self-administration behavior [33].
  • Zacopride (at 0.03 mg/kg and 0.3 mg/kg) remained an effective antiemetic in animals that received a bilateral vagotomy, abolishing emesis in four of eight and two of eight ferrets, respectively [1].
  • 3. The increase in EEG-energy induced by zacopride (10 micrograms, i.c.v.) was blocked by ICS 205-930 (1 microgram, i.c.v.). Neither the 5-HT3 receptor agonist 2-methyl-5-hydroxytryptamine (30 micrograms, i.c.v.) nor the selective 5-HT3 receptor antagonist MDL 72222 (30 micrograms, i.c.v.) had any effect upon rat EEG [34].
  • Neither zacopride nor 8-OH-DPAT reversed etorphine-induced catatonic immobilization [4].
  • Microinjection of serotonin (10 nmol) into the NTS of halothane-anaesthetized, paralyzed and artificially ventilated rats produced an increase in MAP and lumbar sympathetic nerve discharge which could be completely prevented by prior local microinjection of zacopride, a potent serotonin3 antagonist (200 pmol) [35].


  1. Effects of zacopride and BMY25801 (batanopride) on radiation-induced emesis and locomotor behavior in the ferret. King, G.L., Landauer, M.R. J. Pharmacol. Exp. Ther. (1990) [Pubmed]
  2. 5-Hydroxytryptamine3 receptors mediate tachycardia in conscious instrumented dogs. Wilson, H., Coffman, W.J., Cohen, M.L. J. Pharmacol. Exp. Ther. (1990) [Pubmed]
  3. Comparison of the 5-HT3 receptor antagonist properties of ICS 205-930, GR38032F and zacopride. Cohen, M.L., Bloomquist, W., Gidda, J.S., Lacefield, W. J. Pharmacol. Exp. Ther. (1989) [Pubmed]
  4. Zacopride and 8-OH-DPAT reverse opioid-induced respiratory depression and hypoxia but not catatonic immobilization in goats. Meyer, L.C., Fuller, A., Mitchell, D. Am. J. Physiol. Regul. Integr. Comp. Physiol. (2006) [Pubmed]
  5. Lack of effects of 5HT3 receptor antagonists in the social interaction and elevated plus-maze tests of anxiety in the rat. File, S.E., Johnston, A.L. Psychopharmacology (Berl.) (1989) [Pubmed]
  6. 5-HT3 receptor antagonists reverse helpless behaviour in rats. Martin, P., Gozlan, H., Puech, A.J. Eur. J. Pharmacol. (1992) [Pubmed]
  7. Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase. Bard, J.A., Zgombick, J., Adham, N., Vaysse, P., Branchek, T.A., Weinshank, R.L. J. Biol. Chem. (1993) [Pubmed]
  8. Effect of the serotonin-4 receptor agonist zacopride on aldosterone secretion from the human adrenal cortex: in vivo and in vitro studies. Lefebvre, H., Contesse, V., Delarue, C., Soubrane, C., Legrand, A., Kuhn, J.M., Wolf, L.M., Vaudry, H. J. Clin. Endocrinol. Metab. (1993) [Pubmed]
  9. Pharmacological characterization of 5-hydroxytryptamine4(5-HT4) receptors positively coupled to adenylate cyclase in adult guinea pig hippocampal membranes: effect of substituted benzamide derivatives. Bockaert, J., Sebben, M., Dumuis, A. Mol. Pharmacol. (1990) [Pubmed]
  10. Serotonin stimulation of 5-HT4 receptors indirectly enhances in vivo dopamine release in the rat striatum. De Deurwaerdère, P., L'hirondel, M., Bonhomme, N., Lucas, G., Cheramy, A., Spampinato, U. J. Neurochem. (1997) [Pubmed]
  11. An initial three-component pharmacophore for specific serotonin-3 receptor ligands. Rizzi, J.P., Nagel, A.A., Rosen, T., McLean, S., Seeger, T. J. Med. Chem. (1990) [Pubmed]
  12. Comparison of potencies of 5-HT3 receptor antagonists at inhibiting aversive behavior to illumination and the von Bezold-Jarisch reflex in the mouse. Eglen, R.M., Lee, C.H., Khabbaz, M., Fontana, D.J., Daniels, S., Kilfoil, T., Wong, E.H. Neuropharmacology (1994) [Pubmed]
  13. Emesis induced by cisplatin in the ferret as a model for the detection of anti-emetic drugs. Costall, B., Domeney, A.M., Naylor, R.J., Tattersall, F.D. Neuropharmacology (1987) [Pubmed]
  14. 5-HT3 receptor antagonists attenuate cocaine-induced locomotion in mice. Reith, M.E. Eur. J. Pharmacol. (1990) [Pubmed]
  15. LY277359 maleate: a potent and selective 5-HT3 receptor antagonist without gastroprokinetic activity. Cohen, M.L., Bloomquist, W., Gidda, J.S., Lacefield, W. J. Pharmacol. Exp. Ther. (1990) [Pubmed]
  16. Emesis and defecations induced by the 5-hydroxytryptamine (5-HT3) receptor antagonist zacopride in the ferret. King, G.L. J. Pharmacol. Exp. Ther. (1990) [Pubmed]
  17. Studies on the emetic and antiemetic properties of zacopride and its enantiomers. Sancilio, L.F., Pinkus, L.M., Jackson, C.B., Munson, H.R. Eur. J. Pharmacol. (1991) [Pubmed]
  18. Involvement of 5-hydroxytryptamine in the intestinal motor disturbances induced by mast cell degranulation in rats. Bueno, L., Fargeas, M.J., Theodorou, V., Fioramonti, J. Eur. J. Pharmacol. (1991) [Pubmed]
  19. Interaction of S 21007 with 5-HT3 receptors. In vitro and in vivo characterization. Delagrange, P., Emerit, M.B., Merahi, N., Abraham, C., Morain, P., Rault, S., Renard, P., Pfeiffer, B., Guardiola-Lemaître, B., Hamon, M. Eur. J. Pharmacol. (1996) [Pubmed]
  20. The enantiomers of zacopride: an intra-species comparison of their potencies in functional and anxiolytic models. Bill, D.J., Coleman, J., Hallett, I., Middlefell, V.C., Rhodes, K.F., Fletcher, A. Br. J. Pharmacol. (1995) [Pubmed]
  21. Prevention and treatment of the gastric symptoms of radiation sickness. Dubois, A., Fiala, N., Boward, C.A., Bogo, V. Radiat. Res. (1988) [Pubmed]
  22. Quantitative autoradiographic mapping of 5-HT3 receptors in the rat CNS using [125I]iodo-zacopride and [3H]zacopride as radioligands. Laporte, A.M., Koscielniak, T., Ponchant, M., Vergé, D., Hamon, M., Gozlan, H. Synapse (1992) [Pubmed]
  23. 5-HT3 receptor antagonists block cocaine-induced locomotion via a PCPA-sensitive mechanism. Svingos, A.L., Hitzemann, R. Pharmacol. Biochem. Behav. (1992) [Pubmed]
  24. 5-HT receptor subtypes outside the central nervous system. Roles in the physiology of the gut. Gershon, M.D., Wade, P.R., Kirchgessner, A.L., Tamir, H. Neuropsychopharmacology (1990) [Pubmed]
  25. Are there changes in sensitivity to 5-HT3 receptor ligands following chronic diazepam treatment? Andrews, N., File, S.E. Psychopharmacology (Berl.) (1992) [Pubmed]
  26. The 5-HT4 receptor subtype inhibits K+ current in colliculi neurones via activation of a cyclic AMP-dependent protein kinase. Fagni, L., Dumuis, A., Sebben, M., Bockaert, J. Br. J. Pharmacol. (1992) [Pubmed]
  27. (R) and (S) RS 56532: mixed 5-HT3 and 5-HT4 receptor ligands with opposing enantiomeric selectivity. Eglen, R.M., Bonhaus, D.W., Clark, R.D., Johnson, L.G., Lee, C.H., Leung, E., Smith, W.L., Wong, E.H., Whiting, R.L. Neuropharmacology (1994) [Pubmed]
  28. Effect of 5-hydroxytryptamine3 receptor agonists on phosphoinositides hydrolysis in the rat fronto-cingulate and entorhinal cortices. Edwards, E., Harkins, K., Ashby, C.R., Wang, R.Y. J. Pharmacol. Exp. Ther. (1991) [Pubmed]
  29. Effects of 5-HT receptor antagonists on seizure susceptibility and locomotor activity in DBA/2 mice. Semenova, T.P., Ticku, M.K. Brain Res. (1992) [Pubmed]
  30. Effects of serotonergic agents on isolation-induced aggression. White, S.M., Kucharik, R.F., Moyer, J.A. Pharmacol. Biochem. Behav. (1991) [Pubmed]
  31. Stimulation of 5-HT3 receptors in the NTS inhibits the cardiac Bezold-Jarisch reflex response. Sévoz, C., Nosjean, A., Callera, J.C., Machado, B., Hamon, M., Laguzzi, R. Am. J. Physiol. (1996) [Pubmed]
  32. 5-HT3 receptor agonism may be responsible for the emetic effects of zacopride in the ferret. Middlefell, V.C., Price, T.L. Br. J. Pharmacol. (1991) [Pubmed]
  33. Effects of serotonin-3 receptor antagonists on the intracranial self-administration of ethanol within the ventral tegmental area of Wistar rats. Rodd-Henricks, Z.A., McKinzie, D.L., Melendez, R.I., Berry, N., Murphy, J.M., McBride, W.J. Psychopharmacology (Berl.) (2003) [Pubmed]
  34. Zacopride and BRL 24924 induce an increase in EEG-energy in rats. Boddeke, H.W., Kalkman, H.O. Br. J. Pharmacol. (1990) [Pubmed]
  35. Increased sympathetic nerve discharge without alteration in the sympathetic baroreflex response by serotonin3 receptor stimulation in the nucleus tractus solitarius of the rat. Nosjean, A., Franc, B., Laguzzi, R. Neurosci. Lett. (1995) [Pubmed]
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