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Chemical Compound Review

IPSAPIRONE     9,9-dioxo-8-[4-(4-pyrimidin- 2-ylpiperazin...

Synonyms: Ipsapirona, Ipsapironum, Tocris-1869, CHEMBL8412, SureCN79574, ...
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Disease relevance of IPSAPIRONE

  • There were no significant differences in the IPS-induced hypothermia in men and women or between patients with SCH and normal control subjects [1].
  • In both control and ipsapirone-treated (30 mg/kg i.p. 30 minutes after induction of ischemia) animals, the vessel occlusion caused a severe reduction in amplitudes of somatosensory evoked potentials in all areas under record (p less than 0.05) [2].
  • METHODS: Ipsapirone (0.3 mg/kg body weight), or placebo was administered to 30 normal subjects (14 males, 19-74 years and 16 females, 22-69 years) using a randomized, double blind design [3].
  • Adverse experiences that were reported significantly more often for ipsapirone than placebo included asthenia, nausea, dizziness, paresthesias and sweating [4].
  • However, 8-OH-DPAT and ipsapirone differed from clonidine in that their hypotensive action was associated with moderate sympathoinhibition and a profound bradycardia, whereas clonidine caused profound sympathoinhibition and, as it did not increase central vagal tone, only a moderate bradycardia [5].

Psychiatry related information on IPSAPIRONE


High impact information on IPSAPIRONE


Chemical compound and disease context of IPSAPIRONE


Biological context of IPSAPIRONE

  • The present study investigates the effects of the 5-hydroxytryptamine1A agonist ipsapirone on electroencephalography and somatosensory evoked potentials after middle cerebral artery occlusion in the rat [2].
  • In addition, 8-OH-DPAT increased total fluid intake, whereas ipsapirone enhanced total food intake [19].
  • 4. Extracellular recording of the firing rate of 5-hydroxytryptaminergic neurones in the DRN showed that (-)-pindolol blocked, in a concentration-dependent manner, the decrease in firing elicited by 100 nM 5-CT (IC50=598 nM; apparent KB= 131.7 nM) or 100 nM ipsapirone (IC50= 132.5 nM; apparent KB= 124.9 nM) [20].
  • Herein, we investigated whether this treatment promotes tachyphylaxis to the acute neuroendocrine effects of ipsapirone [21].
  • All the drugs used as putative receptor antagonists, as well as PCA, did not change or decreased (ipsapirone) the body temperature in heat-adapted rats.(ABSTRACT TRUNCATED AT 250 WORDS)[22]

Anatomical context of IPSAPIRONE

  • Ipsapirone protected 53% of pyramidal neurons (p less than 0.05) in the CA1 area of the hippocampus from ischemic damage at a dose of 3 mg/kg [23].
  • 8-Hydroxy-2-(di-n-propylamino)tetralin (8OHDPAT) and ipsapirone were injected iv in conscious, freely moving male rats cannulated in the jugular vein [24].
  • Whereas a 30-min restraint stress did not alter the inhibitory influence of ipsapirone on the firing of serotoninergic neurons in the dorsal raphe nucleus, the same session followed by a 24-h isolation produced a significant decrease in the potency of the 5-hydroxytryptamine-1A agonist to inhibit the electrical activity of these cells [25].
  • Similarly, exposure of the animals to novel uncontrolled environmental conditions for 16 h significantly reduced the potency of ipsapirone to decrease the firing rate of serotoninergic neurons in brain stem slices [25].
  • 5-HT, RU-24969 and ipsapirone displaced [3H]-5-HT but not [3H]ketanserin from pigeon brain membranes [26].

Associations of IPSAPIRONE with other chemical compounds

  • These three agonists were also more potent in reducing 5-HTP accumulation in the cortex than in the hippocampus (ED50, 8-OH-DPAT, 14 and 30 microgram/kg; buspirone, 0.42 and 0.63 mg/kg; ipsapirone, 0.44 and 1.26 mg/kg, respectively) [27].
  • 5-HT1A agonists with anxiolytic properties (e.g., buspirone, gepirone, and ipsapirone) display full intrinsic activity at these receptors but are partial agonists at postsynaptic 5-HT1A receptors, which suggests that the latter sites may be devoid of a receptor reserve [28].
  • We determined the effect of chronic fluoxetine and desipramine (DMI) on the hormone response to ipsapirone, a 5-HT1A agonist and a potential anxiolytic drug [29].
  • Using microdialysis, we examined the modifications of 5-HT release induced by the selective 5-HT1A agonist ipsapirone in both neuronal pathways [30].
  • Short term PVN lesions prevented ipsapirone-induced corticosterone and DOI-induced oxytocin responses [31].

Gene context of IPSAPIRONE

  • Two selective 5-HT1A agonists: 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT) and ipsapirone, could not stimulate adenylate cyclase [32].
  • These results contrast with previous studies, which found no effect of ipsapirone on PRL and GH release in humans, but are in accordance with data using other 5-HT1A agonist drugs [33].
  • Oxytocin responses to ipsapirone and DOI, but not m-CPP were markedly attenuated after PVN lesions [34].
  • Here, we investigated the effects of the 5-HT1A receptor partial agonist ipsapirone, which produces behavioral effects and HPA-axis activation, to further characterize the 5-HT receptor subtype-specificity of these disturbances in SAD [35].
  • Furthermore, a approximately 10-fold decrease in the potency of the 5-HT(1A) receptor agonist ipsapirone to inhibit the discharge of serotoninergic neurons in the dorsal raphe nucleus within brainstem slices, and reduced hypothermic response to 8-OH-DPAT, were noted in NK1-/- versus NK1+/+ mice [36].

Analytical, diagnostic and therapeutic context of IPSAPIRONE


  1. 5-HT(1A) receptor dysfunction in female patients with schizophrenia. Lee, M.A., Meltzer, H.Y. Biol. Psychiatry (2001) [Pubmed]
  2. Effects of ipsapirone on spatial and temporal changes in somatosensory evoked potentials after middle cerebral artery occlusion in the rat. Wagener, G., Hielscher, H., Rossberg, C., Wagner, H.J., Bielenberg, G.W. Stroke (1990) [Pubmed]
  3. Low doses of ipsapirone increase growth hormone but not oxytocin secretion in normal male and female subjects. Newman, M.E., Li, Q., Gelfin, Y., Van de Kar, L.D., Lerer, B. Psychopharmacology (Berl.) (1999) [Pubmed]
  4. A placebo-controlled double-blind multicenter trial of two doses of ipsapirone versus diazepam in generalized anxiety disorder. Boyer, W.F., Feighner, J.P. International clinical psychopharmacology. (1993) [Pubmed]
  5. Evidence that the putative 5-HT1A receptor agonists, 8-OH-DPAT and ipsapirone, have a central hypotensive action that differs from that of clonidine in anaesthetised cats. Ramage, A.G., Fozard, J.R. Eur. J. Pharmacol. (1987) [Pubmed]
  6. 5-Hydroxytryptamine1A receptor responsivity in obsessive-compulsive disorder. Comparison of patients and controls. Lesch, K.P., Hoh, A., Disselkamp-Tietze, J., Wiesmann, M., Osterheider, M., Schulte, H.M. Arch. Gen. Psychiatry (1991) [Pubmed]
  7. 5-HT1A receptor responsivity in unipolar depression. Evaluation of ipsapirone-induced ACTH and cortisol secretion in patients and controls. Lesch, K.P., Mayer, S., Disselkamp-Tietze, J., Hoh, A., Wiesmann, M., Osterheider, M., Schulte, H.M. Biol. Psychiatry (1990) [Pubmed]
  8. Behavioural physiology of serotonergic and steroid-like anxiolytics as antistress drugs. Bohus, B., Koolhaas, J.M., Korte, S.M., Bouws, G.A., Eisenga, W., Smit, J. Neuroscience and biobehavioral reviews. (1990) [Pubmed]
  9. Smoking modulates neuroendocrine responses to ipsapirone in patients with panic disorder. Broocks, A., Bandelow, B., Koch, K., Bartmann, U., Kinkelbur, J., Schweiger, U., Hohagen, F., Hajak, G. Neuropsychopharmacology (2002) [Pubmed]
  10. Dissociable hormonal, cognitive and mood responses to neuroendocrine challenge: evidence for receptor-specific serotonergic dysregulation in depressed mood. Riedel, W.J., Klaassen, T., Griez, E., Honig, A., Menheere, P.P., van Praag, H.M. Neuropsychopharmacology (2002) [Pubmed]
  11. Ultrasonic vocalizations in rat pups: effects of serotonergic ligands. Olivier, B., Molewijk, H.E., van der Heyden, J.A., van Oorschot, R., Ronken, E., Mos, J., Miczek, K.A. Neuroscience and biobehavioral reviews. (1998) [Pubmed]
  12. Sleep electroencephalographic response to muscarinic and serotonin1A receptor probes in patients with major depression and in normal controls. Seifritz, E., Gillin, J.C., Rapaport, M.H., Kelsoe, J.R., Bhatti, T., Stahl, S.M. Biol. Psychiatry (1998) [Pubmed]
  13. Behavioral effects of 5-HT receptor ligands in the aversive brain stimulation, elevated plus-maze and learned helplessness tests. Graeff, F.G., Audi, E.A., Almeida, S.S., Graeff, E.O., Hunziker, M.H. Neuroscience and biobehavioral reviews. (1990) [Pubmed]
  14. Effects of 5HT-1A agonists on locomotor and investigatory behaviors in rats differ from those of hallucinogens. Mittman, S.M., Geyer, M.A. Psychopharmacology (Berl.) (1989) [Pubmed]
  15. Profile of action of a novel 5-hydroxytryptamine1A receptor ligand E-4424 to inhibit aversive behavior in the mouse, rat and marmoset. Costall, B., Domeney, A.M., Farre, A.J., Kelly, M.E., Martinez, L., Naylor, R.J. J. Pharmacol. Exp. Ther. (1992) [Pubmed]
  16. The effect of 5-HT1A receptor agonists on locomotor activity in the guinea-pig. Evenden, J.L. Br. J. Pharmacol. (1994) [Pubmed]
  17. Anxiogenic effect of central CCK administration is attenuated by chronic fluoxetine or ipsapirone treatment. To, C.T., Bagdy, G. Neuropharmacology (1999) [Pubmed]
  18. Behavioural and pharmacological characterisation of the canopy stretched attend posture test as a model of anxiety in mice and rats. Grewal, S.S., Shepherd, J.K., Bill, D.J., Fletcher, A., Dourish, C.T. Psychopharmacology (Berl.) (1997) [Pubmed]
  19. Ipsapirone and 8-OH-DPAT reduce ethanol preference in rats: involvement of presynaptic 5-HT1A receptors. Schreiber, R., Opitz, K., Glaser, T., De Vry, J. Psychopharmacology (Berl.) (1993) [Pubmed]
  20. Antagonist properties of (-)-pindolol and WAY 100635 at somatodendritic and postsynaptic 5-HT1A receptors in the rat brain. Corradetti, R., Laaris, N., Hanoun, N., Laporte, A.M., Le Poul, E., Hamon, M., Lanfumey, L. Br. J. Pharmacol. (1998) [Pubmed]
  21. Chronic treatment with an anxiolytic dose of the 5-HT1A agonist ipsapirone does not alter ipsapirone acute neuroendocrine effects. Schmidt, B.H., Chaouloff, F. Psychoneuroendocrinology (1993) [Pubmed]
  22. Hyperthermia induced by m-trifluoromethylphenylpiperazine (TFMPP) or m-chlorophenylpiperazine (m-CPP) in heat-adapted rats. Kłodzińska, A., Chojnacka-Wójcik, E. Psychopharmacology (Berl.) (1992) [Pubmed]
  23. Effects of 5-hydroxytryptamine1A-receptor agonists on hippocampal damage after transient forebrain ischemia in the Mongolian gerbil. Bode-Greuel, K.M., Klisch, J., Horváth, E., Glaser, T., Traber, J. Stroke (1990) [Pubmed]
  24. Changes in anterior pituitary hormone levels after serotonin 1A receptor stimulation. Di Sciullo, A., Bluet-Pajot, M.T., Mounier, F., Oliver, C., Schmidt, B., Kordon, C. Endocrinology (1990) [Pubmed]
  25. Differential effects of stress on presynaptic and postsynaptic 5-hydroxytryptamine-1A receptors in the rat brain: an in vitro electrophysiological study. Laaris, N., Le Poul, E., Laporte, A.M., Hamon, M., Lanfumey, L. Neuroscience (1999) [Pubmed]
  26. 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]
  27. Receptor reserve for 5-hydroxytryptamine1A-mediated inhibition of serotonin synthesis: possible relationship to anxiolytic properties of 5-hydroxytryptamine1A agonists. Meller, E., Goldstein, M., Bohmaker, K. Mol. Pharmacol. (1990) [Pubmed]
  28. Lack of apparent receptor reserve at postsynaptic 5-hydroxytryptamine1A receptors negatively coupled to adenylyl cyclase activity in rat hippocampal membranes. Yocca, F.D., Iben, L., Meller, E. Mol. Pharmacol. (1992) [Pubmed]
  29. Attenuation of hormone responses to the 5-HT1A agonist ipsapirone by long-term treatment with fluoxetine, but not desipramine, in male rats. Li, Q., Brownfield, M.S., Levy, A.D., Battaglia, G., Cabrera, T.M., Van de Kar, L.D. Biol. Psychiatry (1994) [Pubmed]
  30. Differential effects of ipsapirone on 5-hydroxytryptamine release in the dorsal and median raphe neuronal pathways. Casanovas, J.M., Artigas, F. J. Neurochem. (1996) [Pubmed]
  31. Hypothalamic paraventricular nucleus lesions differentially affect serotonin-1A (5-HT1A) and 5-HT2 receptor agonist-induced oxytocin, prolactin, and corticosterone responses. Bagdy, G., Makara, G.B. Endocrinology (1994) [Pubmed]
  32. A nonclassical 5-hydroxytryptamine receptor positively coupled with adenylate cyclase in the central nervous system. Dumuis, A., Bouhelal, R., Sebben, M., Cory, R., Bockaert, J. Mol. Pharmacol. (1988) [Pubmed]
  33. Neuroendocrine and hypothermic effects of 5-HT1A receptor stimulation with ipsapirone in healthy men: a placebo-controlled study. Cleare, A.J., Forsling, M., Bond, A.J. International clinical psychopharmacology. (1998) [Pubmed]
  34. Role of the hypothalamic paraventricular nucleus in 5-HT1A, 5-HT2A and 5-HT2C receptor-mediated oxytocin, prolactin and ACTH/corticosterone responses. Bagdy, G. Behav. Brain Res. (1996) [Pubmed]
  35. Serotonin hypothesis of winter depression: behavioral and neuroendocrine effects of the 5-HT(1A) receptor partial agonist ipsapirone in patients with seasonal affective disorder and healthy control subjects. Schwartz, P.J., Turner, E.H., Garcia-Borreguero, D., Sedway, J., Vetticad, R.G., Wehr, T.A., Murphy, D.L., Rosenthal, N.E. Psychiatry research. (1999) [Pubmed]
  36. 5-hydroxytryptamine (5-HT)1A autoreceptor adaptive changes in substance P (neurokinin 1) receptor knock-out mice mimic antidepressant-induced desensitization. Froger, N., Gardier, A.M., Moratalla, R., Alberti, I., Lena, I., Boni, C., De Felipe, C., Rupniak, N.M., Hunt, S.P., Jacquot, C., Hamon, M., Lanfumey, L. J. Neurosci. (2001) [Pubmed]
  37. Blunted 5-HT1A-receptor agonist-induced corticotropin and cortisol responses after long-term ipsapirone and fluoxetine administration to healthy subjects. Berlin, I., Warot, D., Legout, V., Guillemant, S., Schöllnhammer, G., Puech, A.J. Clin. Pharmacol. Ther. (1998) [Pubmed]
  38. Decreased neuroendocrine responses to meta-chlorophenylpiperazine (m-CPP) but normal responses to ipsapirone in marathon runners. Broocks, A., Meyer, T., George, A., Hillmer-Vogel, U., Meyer, D., Bandelow, B., Hajak, G., Bartmann, U., Gleiter, C.H., Rüther, E. Neuropsychopharmacology (1999) [Pubmed]
  39. Blunted hormone responses to Ipsapirone are associated with trait impulsivity in personality disorder patients. Minzenberg, M.J., Grossman, R., New, A.S., Mitropoulou, V., Yehuda, R., Goodman, M., Reynolds, D.A., Silverman, J.M., Coccaro, E.F., Marcus, S., Siever, L.J. Neuropsychopharmacology (2006) [Pubmed]
  40. A Canadian multicenter study of three fixed doses of controlled-release ipsapirone in outpatients with moderate to severe major depression. Lapierre, Y.D., Silverstone, P., Reesal, R.T., Saxena, B., Turner, P., Bakish, D., Plamondon, J., Vincent, P.M., Remick, R.A., Kroft, C., Payeur, R., Rosales, D., Lam, R., Bologa, M. Journal of clinical psychopharmacology. (1998) [Pubmed]
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