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Chemical Compound Review

quipazine     2-piperazin-1-ylquinoline

Synonyms: Quipazina, Quipazinum, Lopac-Q-1004, Tocris-0629, TPC-A004, ...
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Disease relevance of quipazine


Psychiatry related information on quipazine


High impact information on quipazine

  • We have found that, in contrast to F344/N rats, LEW/N rats had markedly impaired plasma corticotropin and corticosterone responses to SCW, recombinant human interleukin 1 alpha, the serotonin agonist quipazine, and synthetic rat/human corticotropin-releasing hormone [11].
  • This effect was selective for cell type because serotonin or quipazine (100 microM) did not increase prostacyclin synthesis by bovine aortic endothelial cells [12].
  • Qualitative and theoretical quantitative structure-affinity relationship studies were carried out, and the interaction model for the 5-HT3 ligands related to quipazine with their receptor, proposed in part 1 of the present work, was updated to incorporate the latest data [13].
  • Treatment of cells with random, sense, or mismatch oligodeoxynucleotide did not alter the stimulation of PI hydrolysis by quipazine or 5-HT2A receptor number [14].
  • The rate of onset of the inhibitory effect of bath-applied 5-HT was slowed in the presence of (+)-tubocurarine but not in the presence of quipazine [15].

Chemical compound and disease context of quipazine


Biological context of quipazine

  • Compound 5j acted as a 5-HT3 agonist in this assay with an EC50 value close to that reported for quipazine, while 5b was a partial agonist with an EC50 value of about 0.25 nM, and compound 5c possessed antagonist properties with an IC50 value (approximately 8 nM) in the same range as those of previously characterized 5-HT3 receptor antagonists [20].
  • Discriminative stimulus properties of quipazine: mediation by serotonin2 binding sites [21].
  • Quipazine reduces food intake in the rat by activation of 5-HT2-receptors [22].
  • The present study examined the effects of quipazine on mean arterial pressure (MAP), heart rate (HR) and PRA in conscious, chronically catheterized male rats [1].
  • Down-regulation of the protein kinase C isozymes alpha and epsilon by overnight exposure to phorbol-12,13-dibutyrate attenuated the intermediate phase (i.e., after 2-6 hr of agonist exposure) of DOI- and quipazine-induced desensitization [23].

Anatomical context of quipazine

  • Effect of robotic-assisted treadmill training and chronic quipazine treatment on hindlimb stepping in spinally transected rats [24].
  • Involvement of the locus coeruleus in the potentiation of the quipazine-induced head-twitch response by diazepam and beta-adrenoceptor agonists [25].
  • Lesions of intergeniculate leaflet and serotonin afferents to the suprachiasmatic nucleus did not reduce the photic-like effects of quipazine, whereas bilateral enucleation and the subsequent degeneration of the retinohypothalamic tract abolished both the phase-shifting and the FOS-inducing effects of quipazine [26].
  • Quipazine or vehicle was administered to the lumbar spinal cord using an intrathecal cannula [24].
  • However, agonists, quipazine and trifluoromethylphenylpiperazine, with greater reported affinities for 5HT binding sites on rat brain membranes than MK212 were without effect as were the antagonists metergoline, methysergide, cyproheptadine, mianserine and methiothepin [27].

Associations of quipazine with other chemical compounds


Gene context of quipazine

  • The nonspecific 5-HT receptor agonist (and 5-HT2 receptor antagonist) quipazine also induced "wet dog shaking" at doses which suppressed aggression, social interest, and exploration but increased inactive behaviors (sitting and lying) [33].
  • Intrathecal administration of 5-HT3 receptor agonist quipazine (200 mg) abolished nociceptive flexion reflex and alleviated spinal pain syndrome produced by impairment of GABAergic inhibition in the lumbar spinal segments [34].
  • Previous data showed that an acute administration of a 5-HT2 agonist (quipazine) could promote motor function recovery in spinal rats [35].
  • Both beta 1-and beta 2-adrenoceptor agonists potentiated the head-twitch induced by quipazine in sham-operated controls [25].
  • Other serotonergic compounds failed to produce substantial BMY 14802-appropriate responding; such as 5-HT1 agonist I-5-HTP; 5-HT1A/1B agonist RU24969; 5-HT1B/1C agonist m-CPP; 5-HT1C/2 agonist quipazine; 5-HT1C/2 antagonists, metergoline and the atypical antipsychotic clozapine; and 5-HT3 antagonist ondansetron [36].

Analytical, diagnostic and therapeutic context of quipazine


  1. Activation of serotonin2 (5-HT2) receptors by quipazine increases arterial pressure and renin secretion in conscious rats. Alper, R.H., Snider, J.M. J. Pharmacol. Exp. Ther. (1987) [Pubmed]
  2. Evidence for a role for central 5-HT2B as well as 5-HT2A receptors in cardiovascular regulation in anaesthetized rats. Knowles, I.D., Ramage, A.G. Br. J. Pharmacol. (1999) [Pubmed]
  3. Evidence for the role of noradrenaline in some effects of quipazine. Francès, H., Lecrubier, Y., Puech, A.J., Simon, P. Psychopharmacology (Berl.) (1980) [Pubmed]
  4. Serotonin is a directly-acting hyperalgesic agent in the rat. Taiwo, Y.O., Levine, J.D. Neuroscience (1992) [Pubmed]
  5. Antagonism of 5-hydroxytryptamine receptors by quipazine. Lansdown, M.J., Nash, H.L., Preston, P.R., Wallis, D.I., Williams, R.G. Br. J. Pharmacol. (1980) [Pubmed]
  6. Hypophysectomy does not prevent the enhanced monoamine-mediated behavioural responses following repeated electroconvulsive shocks. Nutt, D.J., Smith, S.L., Heal, D.J. Neuropharmacology (1982) [Pubmed]
  7. Methysergide blocks the sleep suppressant action of quipazine in rats. Fornal, C., Radulovacki, M. Psychopharmacology (Berl.) (1982) [Pubmed]
  8. Effects of quipazine and of tryptamine on self-stimulation of median raphé nucleus and of lateral hypothalamus in rats. Broadbent, J., Greenshaw, A.J. Pharmacol. Biochem. Behav. (1985) [Pubmed]
  9. Quipazine has a biphasic effect on slow wave sleep and reduces REM sleep rebound in REM sleep deprived rats. Zak, R., Radulovacki, M. Brain Res. Bull. (1982) [Pubmed]
  10. Comparison of anorexia and motor disruption by cyclazocine and quipazine. Henck, J.W., Rezabek, D.H., Rech, R.H. Pharmacol. Biochem. Behav. (1985) [Pubmed]
  11. Inflammatory mediator-induced hypothalamic-pituitary-adrenal axis activation is defective in streptococcal cell wall arthritis-susceptible Lewis rats. Sternberg, E.M., Hill, J.M., Chrousos, G.P., Kamilaris, T., Listwak, S.J., Gold, P.W., Wilder, R.L. Proc. Natl. Acad. Sci. U.S.A. (1989) [Pubmed]
  12. Serotonin receptor-mediated stimulation of bovine smooth muscle cell prostacyclin synthesis and its modulation by platelet-derived growth factor. Coughlin, S.R., Moskowitz, M.A., Antoniades, H.N., Levine, L. Proc. Natl. Acad. Sci. U.S.A. (1981) [Pubmed]
  13. Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy of arylpiperazine derivatives at the central 5-HT3 receptors. Cappelli, A., Anzini, M., Vomero, S., Canullo, L., Mennuni, L., Makovec, F., Doucet, E., Hamon, M., Menziani, M.C., De Benedetti, P.G., Bruni, G., Romeo, M.R., Giorgi, G., Donati, A. J. Med. Chem. (1999) [Pubmed]
  14. Regulation of serotonin2A receptor expression by an antisense oligodeoxynucleotide. Scalzitti, J.M., Berg, K.A., Kratowicz, S.A., Hensler, J.G. J. Neurochem. (1998) [Pubmed]
  15. Electrophysiological consequences of ligand binding to the desensitized 5-HT3 receptor in mammalian NG108-15 cells. Bartrup, J.T., Newberry, N.R. J. Physiol. (Lond.) (1996) [Pubmed]
  16. Serotonin-induced activation of the network for locomotion in adult spinal rats. Feraboli-Lohnherr, D., Barthe, J.Y., Orsal, D. J. Neurosci. Res. (1999) [Pubmed]
  17. Facilitation of amphetamine-induced hypothermia in mice by GABA agonists and CCK-8. Boschi, G., Launay, N., Rips, R. Br. J. Pharmacol. (1991) [Pubmed]
  18. Central serotonergic systems in the spontaneously hypertensive and Lewis rat strains that differ in the elevated plus-maze test of anxiety. Kulikov, A., Aguerre, S., Berton, O., Ramos, A., Mormede, P., Chaouloff, F. J. Pharmacol. Exp. Ther. (1997) [Pubmed]
  19. Reversal by serotonergic agents of reserpine-induced hyperalgesia in rats. Kulkarni, S.K., Robert, R.K. Eur. J. Pharmacol. (1982) [Pubmed]
  20. Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 1. Mapping the central 5-HT3 receptor binding site by arylpiperazine derivatives. Cappelli, A., Anzini, M., Vomero, S., Mennuni, L., Makovec, F., Doucet, E., Hamon, M., Bruni, G., Romeo, M.R., Menziani, M.C., De Benedetti, P.G., Langer, T. J. Med. Chem. (1998) [Pubmed]
  21. Discriminative stimulus properties of quipazine: mediation by serotonin2 binding sites. Friedman, R.L., Barrett, R.J., Sanders-Bush, E. J. Pharmacol. Exp. Ther. (1984) [Pubmed]
  22. Quipazine reduces food intake in the rat by activation of 5-HT2-receptors. Hewson, G., Leighton, G.E., Hill, R.G., Hughes, J. Br. J. Pharmacol. (1988) [Pubmed]
  23. 5-Hydroxytryptamine2A (5-HT2A) receptor desensitization can occur without down-regulation. Roth, B.L., Palvimaki, E.P., Berry, S., Khan, N., Sachs, N., Uluer, A., Choudhary, M.S. J. Pharmacol. Exp. Ther. (1995) [Pubmed]
  24. Effect of robotic-assisted treadmill training and chronic quipazine treatment on hindlimb stepping in spinally transected rats. de Leon, R.D., Acosta, C.N. J. Neurotrauma (2006) [Pubmed]
  25. Involvement of the locus coeruleus in the potentiation of the quipazine-induced head-twitch response by diazepam and beta-adrenoceptor agonists. Handley, S.L., Singh, L. Neuropharmacology (1986) [Pubmed]
  26. Involvement of the retinohypothalamic tract in the photic-like effects of the serotonin agonist quipazine in the rat. Graff, C., Kohler, M., Pévet, P., Wollnik, F. Neuroscience (2005) [Pubmed]
  27. Analgesia induced by brief footshock is inhibited by 5-hydroxytryptamine but unaffected by antagonists of 5-hydroxytryptamine or by naloxone. Tricklebank, M.D., Hutson, P.H., Curzon, G. Neuropharmacology (1982) [Pubmed]
  28. Habituation of tactile startle is altered by drugs acting on serotonin-2 receptors. Geyer, M.A., Tapson, G.S. Neuropsychopharmacology (1988) [Pubmed]
  29. 5-HT1 and 5-HT2 binding characteristics of some quipazine analogues. Glennon, R.A., Slusher, R.M., Lyon, R.A., Titeler, M., McKenney, J.D. J. Med. Chem. (1986) [Pubmed]
  30. Regulation of noradrenergic coerulean neuronal firing mediated by 5-HT2 receptors: involvement of the prepositus hypoglossal nucleus. Gorea, E., Davenne, D., Lanfumey, L., Chastanet, M., Adrien, J. Neuropharmacology (1991) [Pubmed]
  31. Evidence for 5-HT2 receptor mediation in quipazine anorexia. Shukla, R., MacKenzie-Taylor, D., Rech, R.H. Psychopharmacology (Berl.) (1990) [Pubmed]
  32. Discriminative-stimulus effects of quipazine and l-5-hydroxytryptophan in relation to serotonin binding sites in the pigeon. Walker, E.A., Yamamoto, T., Hollingsworth, P.J., Smith, C.B., Woods, J.H. J. Pharmacol. Exp. Ther. (1991) [Pubmed]
  33. Serotonin receptors and animal models of aggressive behavior. Olivier, B., Mos, J., van Oorschot, R., Hen, R. Pharmacopsychiatry (1995) [Pubmed]
  34. Role of 5-HT3 receptors in the mechanisms of central pain syndrome. Kukushkin, M.L., Igon'kina, S.I. Bull. Exp. Biol. Med. (2003) [Pubmed]
  35. 5-HT1A receptors are involved in short- and long-term processes responsible for 5-HT-induced locomotor function recovery in chronic spinal rat. Antri, M., Mouffle, C., Orsal, D., Barthe, J.Y. Eur. J. Neurosci. (2003) [Pubmed]
  36. Discriminative stimulus characteristics of BMY 14802 in the pigeon. Vanecek, S.A., Essman, W.D., Taylor, D.P., Woods, J.H. J. Pharmacol. Exp. Ther. (1998) [Pubmed]
  37. Rapid agonist-induced internalization of the 5-hydroxytryptamine2A receptor occurs via the endosome pathway in vitro. Berry, S.A., Shah, M.C., Khan, N., Roth, B.L. Mol. Pharmacol. (1996) [Pubmed]
  38. Solubilization, purification, and functional reconstitution of 5-hydroxytryptamine3 receptors from N1E-115 neuroblastoma cells. Lummis, S.C., Martin, I.L. Mol. Pharmacol. (1992) [Pubmed]
  39. Effects of quipazine on pre- and postsynaptic serotonin receptors: single cell studies in the rat CNS. Blier, P., de Montigny, C. Neuropharmacology (1983) [Pubmed]
  40. Serotonergic inhibition of light-induced fos protein expression and extracellular glutamate in the suprachiasmatic nuclei. Selim, M., Glass, J.D., Hauser, U.E., Rea, M.A. Brain Res. (1993) [Pubmed]
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