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Chemical Compound Review

Gepirona     4,4-dimethyl-1-[4-(4- pyrimidin-2...

Synonyms: Gepironum, Variza, Ariza, Gepirone ER, Gepirone HCl, ...
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Disease relevance of Gepirone

  • We tested the full agonists Bay R 1531 and 8-OH-DPAT and the partial agonists ipsapirone and gepirone in the model of transient global ischemia in the Mongolian gerbil [1].
  • The major adverse events were light-headedness, nausea, and insomnia for gepirone and drowsiness and fatigue for diazepam [2].
  • Overall, gepirone ER was well tolerated, with rates of weight gain and sexual dysfunction comparable to placebo [3].
  • The hyperthermia, measured via telemetry, in the "anticipatory" phase prior to defeat and in reaction to threats, was decreased by alcohol, gepirone and diazepam; alcohol and gepirone were also effective in attenuating "anticipatory" tachycardia [4].
  • The anxiolytic-like profile of hyperthermia, tachycardia, USV and defensive behavior in the "anticipatory" phase of the confrontation by alcohol, gepirone and diazepam contrasted with the lack thereof during the more intense reactive phase [4].

Psychiatry related information on Gepirone


High impact information on Gepirone

  • Some of these drugs, including gepirone and other 5-HT1A agonists such as buspirone, have been reported to exert anxiolytic and antidepressive activity in double-blind, placebo-controlled, and comparative trials [9].
  • Twice daily intraperitoneal injection of buspirone (total daily dose of 0.5 and 1 mg/kg), gepirone (0.06 and 0.125 mg/kg), 8-OH dipropylamino-tetralin (8-OH-DPAT) (0.03, 0.06, 0.125, and 0.25 mg/kg), and ipsapirone (TVXQ 7821) (0.03 and 0.06 mg/kg) eliminated escape failures [10].
  • To evaluate long-term efficacy and tolerability of the serotonin 5-HT1A receptor agonist, gepirone extended release (ER), a multicenter, randomized, placebo-controlled relapse prevention study was performed in patients with recurrent major depression (DSM-IV criteria) [11].
  • METHOD: This subgroup analysis was derived from an 8-week, double-blind, placebo-controlled study of gepirone ER in patients with MDD [3].
  • In the hot-plate test, only certain agonists (e.g., 8-OH-DPAT) and partial agonists (e.g., gepirone) elicited antinociception and their actions were not attenuated by 5-HT1A antagonists which, themselves, were inactive in this paradigm [12].

Chemical compound and disease context of Gepirone


Biological context of Gepirone


Anatomical context of Gepirone

  • In contrast, the responsiveness of postsynaptic dorsal hippocampus pyramidal neurons to 5-HT, 8-OH-DPAT, and gepirone was not altered by the 14-day gepirone treatment [22].
  • Anxiolytic drugs, such as the benzodiazepines and the azapirones (ipsapirone, gepirone, buspirone), are well known to affect states of vigilance and to decrease the firing rate of serotoninergic neurones within the dorsal raphe nucleus in rats [23].
  • Formation of 1-PP from gepirone in liver microsomes proceeded with a mean apparent Km ranging from 335 to 677 microM [20].
  • Analysis of small intestinal longitudinal muscle of rats given the ED50 of PmP, ipsapirone, gepirone, buspirone showed that PmP concentrations in the longitudinal muscle (with attached myenteric plexus) fell within a relatively narrow range and were consistent with the appropriate transit scores [24].
  • It was designed to compare the bioavailability of an oral 20-mg gepirone dose (treatment 1) with that obtained after application of the same dose by gastric intubation to the distal (treatment 2) and proximal (treatment 3) regions of the small intestine, and after 4 consecutive 5-mg gepirone doses given orally at hourly intervals (treatment 4) [25].

Associations of Gepirone with other chemical compounds

  • The 5-HT1A agonist properties of gepirone were used to test for effects on serum cortisol levels in humans, 90 min after a 10 mg oral dose [26].
  • Ipsapirone-induced acceleration of DA turnover persisted after the selective degeneration of serotoninergic neurons by intraraphe 5,7-dihydroxytryptamine infusion, and could be reproduced by i.p. administration of other 5-HT1A agonists like buspirone and gepirone, but not 8-OH-DPAT [27].
  • The same maximal drop in body temperature (approximately 2.5 degrees C) was elicited by all three agonists, 8-OH-DPAT being the most potent (EC50 = 0.05 mg/kg), followed by gepirone (1.8 mg/kg) and (+) S-20499 (8 mg/kg) [28].
  • In contrast, acute doses of gepirone had little effect on rates of cocaine self-administration, while disruptions in food consumption and changes in the within-session pattern of cocaine self-administration were obtained at the highest dose of gepirone tested (1.0 mg/kg) [29].
  • The results obtained suggest that the anti-immobility effect of gepirone is mediated by activation of 5-HT1A receptors, most probably located postsynaptically and that dopamine may be involved in this action [30].

Gene context of Gepirone


Analytical, diagnostic and therapeutic context of Gepirone


  1. 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]
  2. Gepirone and diazepam in generalized anxiety disorder: a placebo-controlled trial. Rickels, K., Schweizer, E., DeMartinis, N., Mandos, L., Mercer, C. Journal of clinical psychopharmacology. (1997) [Pubmed]
  3. Gepirone extended-release treatment of anxious depression: evidence from a retrospective subgroup analysis in patients with major depressive disorder. Alpert, J.E., Franznick, D.A., Hollander, S.B., Fava, M. The Journal of clinical psychiatry. (2004) [Pubmed]
  4. Alcohol, anxiolytics and social stress in rats. Tornatzky, W., Miczek, K.A. Psychopharmacology (Berl.) (1995) [Pubmed]
  5. Gepirone and the treatment of panic disorder: an open study. Pecknold, J.C., Luthe, L., Scott-Fleury, M.H., Jenkins, S. Journal of clinical psychopharmacology. (1993) [Pubmed]
  6. Gepirone in anxiety: a pilot study. Csanalosi, I., Schweizer, E., Case, W.G., Rickels, K. Journal of clinical psychopharmacology. (1987) [Pubmed]
  7. A review of the efficacy and tolerability of immediate-release and extended-release formulations of gepirone. Robinson, D.S., Sitsen, J.M., Gibertini, M. Clinical therapeutics. (2003) [Pubmed]
  8. Modification of sexual behavior of Long-Evans male rats by drugs acting on the 5-HT1A receptor. Rehman, J., Kaynan, A., Christ, G., Valcic, M., Maayani, S., Melman, A. Brain Res. (1999) [Pubmed]
  9. Is there a role for 5-HT1A agonists in the treatment of depression? Blier, P., Ward, N.M. Biol. Psychiatry (2003) [Pubmed]
  10. Reversal of helpless behavior in rats by putative 5-HT1A agonists. Giral, P., Martin, P., Soubrié, P., Simon, P. Biol. Psychiatry (1988) [Pubmed]
  11. Relapse prevention with gepirone ER in outpatients with major depression. Keller, M.B., Ruwe, F.J., Janssens, C.J., Sitsen, J.M., Jokinen, R., Janczewski, J. Journal of clinical psychopharmacology. (2005) [Pubmed]
  12. Serotonin and pain: evidence that activation of 5-HT1A receptors does not elicit antinociception against noxious thermal, mechanical and chemical stimuli in mice. Millan, M.J. Pain (1994) [Pubmed]
  13. Effects of 5-HT1A selective anxiolytics on lordosis behavior: interactions with progesterone. Mendelson, S.D., Gorzalka, B.B. Eur. J. Pharmacol. (1986) [Pubmed]
  14. Influence of housing conditions on the effects of serotonergic drugs on feeding behavior in non-deprived rats. Silva, R.C., Santos, N.R., Brandão, M.L. Neuropsychobiology (2003) [Pubmed]
  15. 5-HT2 receptor blockade by ICI 170,809 does not affect the inhibitory effect of the 5-HT1A receptor ligand gepirone on neuroleptic-induced catalepsy. Pires, J.G., Silva, S.R., Futuro-Neto, H.A. Braz. J. Med. Biol. Res. (1994) [Pubmed]
  16. Attenuation of the fentanyl-induced muscle rigidity by the selective 5HT1A agonist 8-OH-DPAT. Jaros, T., Kolasiewicz, W. Polish journal of pharmacology. (1995) [Pubmed]
  17. Neuroendocrine effects of azapirones. Cowen, P.J., Anderson, I.M., Grahame-Smith, D.G. Journal of clinical psychopharmacology. (1990) [Pubmed]
  18. Neurochemistry and neurophysiology of buspirone and gepirone: interactions at presynaptic and postsynaptic 5-HT1A receptors. Yocca, F.D. Journal of clinical psychopharmacology. (1990) [Pubmed]
  19. Influence of taste and food texture on the feeding responses induced by 8-OH-DPAT and gepirone. Fletcher, P.J., Zack, M.H., Coscina, D.V. Psychopharmacology (Berl.) (1991) [Pubmed]
  20. Gepirone and 1-(2-pyrimidinyl)-piperazine in vitro: human cytochromes mediating transformation and cytochrome inhibitory effects. von Moltke, L.L., Greenblatt, D.J., Grassi, J.M., Granda, B.W., Fogelman, S.M., Harmatz, J.S., Kramer, S.J., Fabre, L.F., Shader, R.I. Psychopharmacology (Berl.) (1998) [Pubmed]
  21. Effect of food on the bioavailability of gepirone in humans. Tay, L.K., Sciacca, M.A., Sostrin, M.B., Farmen, R.H., Pittman, K.A. Journal of clinical pharmacology. (1993) [Pubmed]
  22. Differential effect of gepirone on presynaptic and postsynaptic serotonin receptors: single-cell recording studies. Blier, P., de Montigny, C. Journal of clinical psychopharmacology. (1990) [Pubmed]
  23. Central action of 5-HT3 receptor ligands in the regulation of sleep-wakefulness and raphe neuronal activity in the rat. Adrien, J., Tissier, M.H., Lanfumey, L., Haj-Dahmane, S., Jolas, T., Franc, B., Hamon, M. Neuropharmacology (1992) [Pubmed]
  24. The alpha 2-adrenoceptor antagonist activity of ipsapirone and gepirone is mediated by their common metabolite 1-(2-pyrimidinyl)-piperazine (PmP). Bianchi, G., Caccia, S., Della Vedova, F., Garattini, S. Eur. J. Pharmacol. (1988) [Pubmed]
  25. The site of gastrointestinal absorption of gepirone in humans. Tay, L.K., Dixon, F., Sostrin, M.B., Barr, W.H., Farmen, R.H., Pittman, K.A. Journal of clinical pharmacology. (1992) [Pubmed]
  26. Cortisol and growth hormone responses to the 5-HT1A agonist gepirone in depressed patients. Rausch, J.L., Stahl, S.M., Hauger, R.L. Biol. Psychiatry (1990) [Pubmed]
  27. Alterations of central serotonin and dopamine turnover in rats treated with ipsapirone and other 5-hydroxytryptamine1A agonists with potential anxiolytic properties. Hamon, M., Fattaccini, C.M., Adrien, J., Gallissot, M.C., Martin, P., Gozlan, H. J. Pharmacol. Exp. Ther. (1988) [Pubmed]
  28. Differential induction of 5-HT1A-mediated responses in vivo by three chemically dissimilar 5-HT1A agonists. Scott, P.A., Chou, J.M., Tang, H., Frazer, A. J. Pharmacol. Exp. Ther. (1994) [Pubmed]
  29. Effects of buspirone and gepirone on i.v. cocaine self-administration in rhesus monkeys. Gold, L.H., Balster, R.L. Psychopharmacology (Berl.) (1992) [Pubmed]
  30. Involvement of 5-HT1A receptors in the antidepressant-like activity of gepirone in the forced swimming test in rats. Chojnacka-Wójcik, E., Tatarczyńska, E., Gołembiowska, K., Przegaliński, E. Neuropharmacology (1991) [Pubmed]
  31. The role of serotonergic mechanisms in inhibition of isolation-induced aggression in male mice. Sánchez, C., Arnt, J., Hyttel, J., Moltzen, E.K. Psychopharmacology (Berl.) (1993) [Pubmed]
  32. 5-HT1A receptor-mediated regulation of mitogen-activated protein kinase phosphorylation in rat brain. Chen, J., Shen, C., Meller, E. Eur. J. Pharmacol. (2002) [Pubmed]
  33. Metabolism of the newest antidepressants: comparisons with related predecessors. Caccia, S. IDrugs : the investigational drugs journal. (2004) [Pubmed]
  34. Effects of blockade of 5-HT2 receptors and activation of 5-HT1A receptors on the exploratory activity of rats in the elevated plus-maze. Motta, V., Maisonnette, S., Morato, S., Castrechini, P., Brandão, M.L. Psychopharmacology (Berl.) (1992) [Pubmed]
  35. Evidence that corticotropin-releasing factor within the extended amygdala mediates the activation of tryptophan hydroxylase produced by sound stress in the rat. Boadle-Biber, M.C., Singh, V.B., Corley, K.C., Phan, T.H., Dilts, R.P. Brain Res. (1993) [Pubmed]
  36. Abuse potential of buspirone and related drugs. Balster, R.L. Journal of clinical psychopharmacology. (1990) [Pubmed]
  37. Establishing the maximum tolerated dose of lesopitron in patients with generalized anxiety disorder: a bridging study. Sramek, J.J., Fresquet, A., Marion-Landais, G., Hourani, J., Jhee, S.S., Martinez, L., Jensen, C.M., Bolles, K., Carrington, A.T., Cutler, N.R. Journal of clinical psychopharmacology. (1996) [Pubmed]
  38. The effects of gepirone on neuroendocrine function and temperature in humans. Anderson, I.M., Cowen, P.J., Grahame-Smith, D.G. Psychopharmacology (Berl.) (1990) [Pubmed]
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