Short communicationThe effects of intraventricular administration of eltoprazine, 1-(3-trifluoromethylphenyl) piperazine hydrochloride and 8-hydroxy-2-(di-n-propylamino) tetralin on resident intruder aggression in the rat
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Cited by (52)
The neurobiology of offensive aggression: Revealing a modular view
2015, Physiology and BehaviorCitation Excerpt :In contrast, 5-HT1B receptor agonists enhanced the threshold for inducing aggression indicating a differential role for both 5-HT1 receptors [166]. Further work has indicated that this anti-aggressive activity of 5-HT1B receptor agonists is predominantly mediated by postsynaptic 5-HT1B receptors [167–169]. Although the findings of de Boer et al. [156] and Olivier et al. [166] seem somewhat contradictory, the presynaptic 5-HT1A autoreceptor is primarily functioning in the regulation of the firing activity of serotonergic neurons and it can be hypothesized that adaptation of individual animals to certain strategies (either high or low aggressive) is associated with adaptations in the autoregulation of serotonergic activity leading to a changed serotonergic tone in the system.
Serotonin: A never-ending story
2015, European Journal of PharmacologyCitation Excerpt :Lesioning the raphé nuclei with the serotonergic neurotoxin 5,7- dihydroxytryptamine (5,7-DHT) which destroys the presynaptic autoreceptors but leaves the postsynaptic heteroreceptors (relatively) unaffected, had an aggression-reducing effect on itself, but in these animals eltoprazine still had an anti-aggressive effect, strongly suggesting that the serenic activity is due to postsynaptic mediated activation of 5-HT1B heteroreceptors (Sijbesma et al., 1991). Similarly, eltoprazine injection in the ventricles, aiming for postsynaptic 5-HT1B receptors had an anti-aggressive effect, whereas direct raphé injections, aimed at presynaptic 5-HT1B autoreceptors were ineffective (Mos et al., 1992, 1993). A big dogma in the relationship between serotonin and aggression is still that 5-HT inhibits aggression (Yanowich and Coccaro, 2011).
The role of the serotonergic system at the interface of aggression and suicide
2013, NeuroscienceCitation Excerpt :Further studies will be needed to elucidate the nature of the multiple discrepancies emerging from the preclinical and clinical literature, as well as the putative roles of pre- and post-synaptic 5-HT1A receptors in the regulation of violent and suicidal behaviours, also with respect to multiple comorbid entities. In rodents, activation of 5-HT1B receptors induces a marked reduction of escalated aggression in a highly specific fashion, which appears to be dissociated from alterations of exploration, locomotion and anxiety-related behaviours (Miczek et al., 1989; Sijbesma et al., 1990; Mos et al., 1992; Bell et al., 1995; Fish et al., 1999; de Almeida et al., 2001; Muehlenkamp and Gutierrez, 2004). The systemic effects of 5-HT1B receptor agonists are reproduced by microinjections of these compounds in the ventral OFC and raphe nuclei, but not infralimbic PFC (De Almeida et al., 2006; Bannai et al., 2007; Centenaro et al., 2008).
5-HT1 receptor agonists for the treatment of L-DOPA-induced dyskinesia: From animal models to clinical investigation
2013, Basal GangliaCitation Excerpt :One promising candidate may be eltoprazine, a mixed 5-HT1A/B agonist developed by Solvay for the treatment of aggression. This drug exhibited a safe toxicological profile and lack of serious side effects [49,50] and is currently in use in a clinical trial in patients with ADHD (ClinicalTrials.gov Identifier: NCT01266174). We have recently shown that eltoprazine is highly effective in blocking LID both in 6-OHDA-lesioned rats and MPTP-treated macaques, although this effect is accompanied by a partial loss of the L-DOPA therapeutic efficacy [51].
Risperidone Exerts Potent Anti-aggressive Effects in a Developmentally Immature Animal Model of Escalated Aggression
2007, Biological PsychiatryCitation Excerpt :A wealth of data supports an inverse relationship between 5HT activity and aggression (Brown et al. 1979, 1982; Higley et al. 1992; Kyes et al. 1995; Mehlman et al. 1994; Miczek et al. 1974; Olivier et al. 1989; Vergnes et al. 1988), and manipulations that elevate 5HT (Auerbach et al. 1989; Ferris 1996; Guan and McBride 1988; Perry and Hughes 1992) serve to suppress aggression (Dalta et al. 1991; Molina et al. 1987; Ogren et al. 1980; Olivier et al. 1989; Sanchez and Hyttel 1994; Villalba et al. 1997). The importance of specific 5HT receptors, namely the 5HT 1A, 1B, and 2A subtype receptors, as mediators of the aggressive response has been demonstrated (Albonetti et al. 1996; Bell et al. 1995; Cologer-Clifford et al. 1997; de Boer et al. 1999; Ferris et al. 1999; Fish et al. 1999; Joppa et al. 1997; McMillen et al. 1987; Miczek et al. 1998; Mos et al. 1992; Olivier et al. 1989, 1995; Pfeffer et al. 1997; Ratey et al. 1991; Ricketts et al. 1994; Sakaue et al. 2002; Sanchez et al. 1993; Sanchez and Hyttel 1994; Saudou et al. 1994; Sijbesma et al. 1990, 1991; Verhoeven and Tuinier 1996; White et al. 1991). For instance, activation of 5HT2A receptors with selective 5HT2A agonists increase aggressive behavior (Sakaue et al. 2002), whereas blockade using selective 5HT2A antagonists and mixed 5HT2A and DA D2 receptor antagonists reduces aggression (Sakaue et al. 2002; Sanchez et al. 1993; Shih et al. 1999; Skrebuhhova-Malmros et al. 2000).