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Zacopride

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Zacopride
Clinical data
ATC code
  • none
Identifiers
  • 4-amino-5-chloro-2-methoxy-N-(quinuclidin-3-yl)benzamide
CAS Number
PubChemCID
IUPHAR/BPS
ChemSpider
UNII
ChEBI
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC15H20ClN3O2
Molar mass309.79 g·mol−1
3D model (JSmol)
  • COC1=CC(=C(C=C1C(=O)NC2CN3CCC2CC3)Cl)N
  • 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) ☒N
  • Key:FEROPKNOYKURCJ-UHFFFAOYSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

Zacopride is a potentantagonist at the5-HT3receptor[1] and anagonist at the5-HT4 receptor.[2] It hasanxiolytic[3] andnootropic effects in animal models,[4] with the (R)-(+)-enantiomer being the more active form.[5] It also hasantiemetic[6] and pro-respiratory effects, both reducingsleep apnea[7] and reversingopioid-inducedrespiratory depression in animal studies.[8] Early animal trials have also revealed that administration of zacopride can reduce preference for and consumption of ethanol.[9]

Zacopride was found to significantly increasealdosterone levels in human subjects for 180 minutes at a dose of 400 micrograms. It is thought to do this by stimulating the 5-HT4 receptors on the adrenal glands. Zacopride also stimulated aldosterone secretion when applied to human adrenal glandsin vitro. No significant changes were observed inrenin,ACTH, orcortisol levels.[2]

Zacopride has been tested in clinical trials for the treatment ofschizophrenia, but was found unsuccessful.[10]

References

[edit]
  1. ^Smith WW, Sancilio LF, Owera-Atepo JB, Naylor RJ, Lambert L (April 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.S2CID 32862252.
  2. ^abLefebvre H, Contesse V, Delarue C, Soubrane C, Legrand A, Kuhn JM, et al. (December 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/jcem.77.6.8263156.PMID 8263156.
  3. ^Costall B, Domeney AM, Gerrard PA, Kelly ME, Naylor RJ (April 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.S2CID 1083706.
  4. ^Fontana DJ, Daniels SE, Eglen RM, Wong EH (March 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.S2CID 12818436.
  5. ^Young R, Johnson DN (August 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.
  6. ^Yamakuni H, Nakayama H, Matsui S, Imazumi K, Matsuo M, Mutoh S (May 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.
  7. ^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.S2CID 11848748.
  8. ^Meyer LC, Fuller A, Mitchell D (February 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.S2CID 224414.
  9. ^Knapp DJ, Pohorecky LA (April 1992). "Zacopride, a 5-HT3 receptor antagonist, reduces voluntary ethanol consumption in rats".Pharmacology, Biochemistry, and Behavior.41 (4):847–50.doi:10.1016/0091-3057(92)90237-A.PMID 1594653.S2CID 45436887.
  10. ^Newcomer JW, Faustman WO, Zipursky RB, Csernansky JG (September 1992). "Zacopride in schizophrenia: a single-blind serotonin type 3 antagonist trial".Archives of General Psychiatry.49 (9):751–2.doi:10.1001/archpsyc.1992.01820090079013.PMID 1514881.
Otherrespiratory system products (R07)
Lung surfactants
Respiratory stimulants
5-HT4 receptor agonists
Other agents for treating respiratory depression
5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT3–7
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
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