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Chemical Compound Review

Eltoprazina     1-(7,10- dioxabicyclo[4.4.0]deca- 1,3,5...

Synonyms: Eltoprazine, Eltoprazinum, CHEMBL282614, SureCN177715, ANW-72449, ...
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Disease relevance of Eltoprazine

  • At postsynaptic 5-HT1A receptors mediating hypothermia, eltoprazine, WY 48,723, MDL 72832 and tandospirone are agonists, zalospirone is a partial agonist and (-)-tertatolol, WAY 100,135, MDL 73005 EF and SDZ 216-525 are antagonists [1].

Psychiatry related information on Eltoprazine


High impact information on Eltoprazine

  • A series of unsubstituted and substituted succinimido, maleimido, and glutarimidoethyl derivatives of eltoprazine (3) was synthesized and tested for affinity for the 5-HT1A receptor in rat brain homogenates [6].
  • The virtual total suppression of REM sleep (0.4%, 4.0 mg/kg) and PGO wave activity (2 to 4 mg/kg) in exchange for increasing amounts of non-REM (NREM) slow-wave sleep was a dose-dependent function of the amount of eltoprazine administered [3].
  • The serotonergic agonist, eltoprazine, behaved as a partial agonist (Emax = 52.7%) at RGlow membranes but virtually as a full agonist (Emax = 93.2%) at RGhigh membranes, relative to 5-HT (= 100%) [7].
  • The eltoprazine cue partially generalized to the cues of the 5-HT1a agonists flesinoxan and buspirone, (m-CPP), the 5-HT1b/1c agonist 1,3-chlorophenyl-piperazine dihydrochloride and the 5-HT1c/2 antagonist mesulergine, and did not generalize to the 5-HT2/1c agonist DOI [8].
  • In this study we report the effects of eltoprazine, a phenylpiperazine derivative with high affinity for 5-hydroxytryptamine1 (5HT1) binding sites, on membrane properties of hippocampal neurons [9].

Biological context of Eltoprazine

  • Pharmacokinetics of eltoprazine in healthy male subjects after single dose oral and intravenous administration [10].
  • Furthermore, GTP did not affect the competition for [125I]ICYP binding by the 5-HT1-antagonist methiothepin, whereas it did significantly reduce the displacement by eltoprazine, resulting in an almost twofold increase in IC50 values [11].
  • The kinetics, safety and tolerability of eltoprazine hydrochloride were studied in an open, cross-over, partially randomised design after single oral (8 mg) and intravenous (3 and 8 mg) doses to 12 healthy male subjects [10].
  • 8-OH-DPAT and flesinoxan (full agonists); ipsapirone (selective partial agonist) and eltoprazine (non selective partial agonist), all induced a dose-dependent reduction in core body temperature, which was maximal 30 min subsequent to administration [12].
  • It was shown that the absorption of eltoprazine from the gastro-intestinal tract was complete, and that absolute bioavailability was 100% [13].

Anatomical context of Eltoprazine

  • Within the amygdala, but not in other structures, the quantitative autoradiographic analysis of the 5-HT2C binding sites showed a differential effect: mianserin treatment induced a decrease in the number of these sites, while eltoprazine treatment resulted in an increase [14].
  • Eltoprazine (1 microM) inhibits the forskolin stimulated c-AMP production in hippocampus slices of the rat, indicating an agonistic action on the 5-HT1A receptor [15].

Associations of Eltoprazine with other chemical compounds

  • As TFMPP has a significantly lower affinity for 5-HT1A receptors than 8-OH-DPAT or eltoprazine, the lack of effect of TFMPP supports this view [16].
  • The data indicate that the anti-aggressive drug eltoprazine preferentially binds to 5-HT1A and 5-HT1B receptor sites and that this interaction is modulated by guanine nucleotides [11].
  • Substitution for 8-OH-DPAT by eltoprazine and RU 24969, which does not occur in rats, provides in vivo support for the suggestion that the absence of a 5-HT1B receptor in the pigeon allows more complete expression of 5-HT1A-mediated effects [17].

Gene context of Eltoprazine

  • Eltoprazine, a mixed 5-HT1A/B agonist, and meta-trifluoro-methylphenyl-piperazine HCl (TFMPP), a more selective 5-HT1B agonist, specifically decrease aggressive behavior in several animal species and situations in both sexes without detriment to other social, exploratory, or motoric activities [18].
  • The pharmacological and anatomical data indicate that eltoprazine binds to 5-HT1A, 5-HT1B and to a lesser extent to 5-HT1C binding sites in the rat brain [19].
  • In spite of this, neither mianserin- nor eltoprazine-treated rats displayed an alteration in the 5-HT2C receptor mRNA levels in the brain regions examined [14].
  • The results suggest that the aggression-modulating effects of eltoprazine, as well as other drugs, may be mediated in part by their effects on normal olfactory function [20].

Analytical, diagnostic and therapeutic context of Eltoprazine


  1. Induction of hypothermia as a model of 5-hydroxytryptamine1A receptor-mediated activity in the rat: a pharmacological characterization of the actions of novel agonists and antagonists. Millan, M.J., Rivet, J.M., Canton, H., Le Marouille-Girardon, S., Gobert, A. J. Pharmacol. Exp. Ther. (1993) [Pubmed]
  2. Eltoprazine for aggression in schizophrenia and mental retardation. Tiihonen, J., Hakola, P., Paanila, J., Turtiainen, M. Lancet (1993) [Pubmed]
  3. Dose-related suppression of REM sleep and PGO waves by the serotonin-1 agonist eltoprazine. Quattrochi, J.J., Mamelak, A.N., Binder, D., Williams, J., Hobson, J.A. Neuropsychopharmacology (1993) [Pubmed]
  4. Dynamic suppression of REM sleep by parenteral administration of the serotonin-1 agonist eltoprazine. Quattrochi, J.J., Mamelak, A., Binder, D.K., Williams, J., Rittenhouse, C., Hobson, J.A. Sleep. (1992) [Pubmed]
  5. Effects of eltoprazine hydrochloride on exploratory behavior and social attraction in mice. Kemble, E.D., Gibson, B.M., Rawleigh, J.M. Pharmacol. Biochem. Behav. (1991) [Pubmed]
  6. A series of N4-imidoethyl derivatives of 1-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazine as 5-HT1A receptor ligands: synthesis and structure-affinity relationships. van Steen, B.J., van Wijngaarden, I., Tulp, M.T., Soudijn, W. J. Med. Chem. (1995) [Pubmed]
  7. Agonist and inverse agonist efficacy at human recombinant serotonin 5-HT1A receptors as a function of receptor:G-protein stoichiometry. Newman-Tancredi, A., Conte, C., Chaput, C., Verrièle, L., Millan, M.J. Neuropharmacology (1997) [Pubmed]
  8. Discriminative stimulus properties of the serotonergic compound eltoprazine. Ybema, C.E., Slangen, J.L., Olivier, B., Mos, J. J. Pharmacol. Exp. Ther. (1992) [Pubmed]
  9. Eltoprazine suppresses hyperpolarizing responses to serotonin in rat hippocampus. Joëls, M., Pennartz, C.M., Sijbesma, H., Schipper, J. J. Pharmacol. Exp. Ther. (1990) [Pubmed]
  10. Pharmacokinetics of eltoprazine in healthy male subjects after single dose oral and intravenous administration. Raghoebar, M., Mak, M., Cournot, A., Pistorius, M.C., Van Harten, J., Roseboom, H. British journal of clinical pharmacology. (1990) [Pubmed]
  11. The anti-aggressive drug eltoprazine preferentially binds to 5-HT1A and 5-HT1B receptor subtypes in rat brain: sensitivity to guanine nucleotides. Sijbesma, H., Schipper, J., De Kloet, E.R. Eur. J. Pharmacol. (1990) [Pubmed]
  12. Comparative effects of serotonergic agonists with varying efficacy at the 5-HT(1A) receptor on core body temperature: modification by the selective 5-HT(1A) receptor antagonist WAY 100635. Cryan, J.F., Kelliher, P., Kelly, J.P., Leonard, B.E. J. Psychopharmacol. (Oxford) (1999) [Pubmed]
  13. Pharmacokinetics of eltoprazine in healthy subjects. van Harten, J., Mathlener, I.S., Raghoebar, M. Drug metabolism and drug interactions. (1990) [Pubmed]
  14. Chronic mianserin or eltoprazine treatment in rats: effects on the elevated plus-maze test and on limbic 5-HT2C receptor levels. Rocha, B., Rigo, M., Di Scala, G., Sandner, G., Hoyer, D. Eur. J. Pharmacol. (1994) [Pubmed]
  15. Neurochemical profile of eltoprazine. Schipper, J., Tulp, M.T., Sijbesma, H. Drug metabolism and drug interactions. (1990) [Pubmed]
  16. The effects of dorsal raphe administration of eltoprazine, TFMPP and 8-OH-DPAT on resident intruder aggression in the rat. Mos, J., Olivier, B., Poth, M., Van Oorschot, R., Van Aken, H. Eur. J. Pharmacol. (1993) [Pubmed]
  17. Discriminative stimulus effects of 8-OH-DPAT in pigeons: antagonism studies with the putative 5-HT1A receptor antagonists BMY 7378 and NAN-190. Barrett, J.E., Gleeson, S. Eur. J. Pharmacol. (1992) [Pubmed]
  18. Brain 5-HT and inhibition of aggressive behavior in animals: 5-HIAA and receptor subtypes. Miczek, K.A., Mos, J., Olivier, B. Psychopharmacology bulletin. (1989) [Pubmed]
  19. Eltoprazine, a drug which reduces aggressive behaviour, binds selectively to 5-HT1 receptor sites in the rat brain: an autoradiographic study. Sijbesma, H., Schipper, J., de Kloet, E.R. Eur. J. Pharmacol. (1990) [Pubmed]
  20. Effects of eltoprazine hydrochloride on reactivity to conspecific or novel odors and activity. Ostrem, J.L., Rawleigh, J.M., Kemble, E.D. Pharmacol. Biochem. Behav. (1992) [Pubmed]
  21. Postsynaptic 5-HT1 receptors and offensive aggression in rats: a combined behavioural and autoradiographic study with eltoprazine. Sijbesma, H., Schipper, J., de Kloet, E.R., Mos, J., van Aken, H., Olivier, B. Pharmacol. Biochem. Behav. (1991) [Pubmed]
  22. Dose-proportionality of eltoprazine. Pharmacokinetics of single oral doses in healthy subjects. de Vries, M.H., de Koning, P., Floot, H.L., Grahnén, A., Eckernäs, S.A., Raghoebar, M., Dahlström, B., Ekman, L. Eur. J. Clin. Pharmacol. (1991) [Pubmed]
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