GR 127935 and (+)-WAY 100135 do not affect TFMPP-induced inhibition of 5-HT synthesis in the midbrain and hippocampus of Wistar-Kyoto rats

Chaouloff, Francis; Aguerre, Sylvie; Mormède, Pierre

doi:10.1016/s0028-3908(98)00107-5

Cited by 14 publications

(6 citation statements)

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“…They are probably complex results of the drug characteristics and actions via multiple receptors, in addition to the effect of the 5‐HT releasing potential of TFMPP (Auerbach et al . 1991) and the actions on 5‐HT synthesis by non‐5‐HT mechanisms (Chaouloff et al . 1998).…”

Section: Discussionmentioning

confidence: 99%

“…1993). In fact, this enhancing action of TFMPP is prevented by a 5‐HT reuptake inhibitor, but not by 5‐HT 1B antagonists, suggesting that there are TFMPP actions on 5‐HT synthesis by non‐5‐HT mechanisms (Chaouloff et al . 1998).…”

Section: Discussionmentioning

confidence: 99%

“…However, it has been shown that TFMPP, mCPP and RU 24969, all preferential 5-HT 1B agonists, increase 5-HT release in microdialysis studies in vivo via an action independent of the terminal 5-HT 1B autoreceptor (Auerbach et al 1991;Baumann et al 1993). In fact, this enhancing action of TFMPP is prevented by a 5-HT reuptake inhibitor, but not by 5-HT 1B antagonists, suggesting that there are TFMPP actions on 5-HT synthesis by non-5-HT mechanisms (Chaouloff et al 1998). Conse- Fig.…”

Section: Figmentioning

confidence: 98%

“…Because there is no quantitative data on the pre-and postsynaptic distribution of 5-HT 1B sites, it is not possible, at this time, to provide a more definitive description of the mechanism of these differences. They are probably complex results of the drug characteristics and actions via multiple receptors, in addition to the effect of the 5-HT releasing potential of TFMPP (Auerbach et al 1991) and the actions on 5-HT synthesis by non-5-HT mechanisms (Chaouloff et al 1998). The observation that TFMPP, but not CGS12066B, decreased 5-HT synthesis in non-cortical areas, but not in some cortical areas, in an acute treatment may appear as paradoxical because these drugs consistently attenuate 5-HTP accumulation in the cortex (Hjorth et al 1995;Moret and Briley 1997).…”

Section: Figmentioning

confidence: 99%

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Effects of serotine receptors agonists, TFMPP and CGS12066B, on regional serotonin synthesis in the rat brain: an autoradiographic study

Tohyama

Yamane

Merid

et al. 2002

Journal of Neurochemistry

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The effects of acute and repeat administration of the serotonin (5-HT) 1 agonists TFMPP [N-(3-trifluoromethyl)phenylpiperazine hydrochloride] and CGS12066B [7-trifluoromethyl-4-(4-methyl-1-piperazinyl)pyrrolo[1,2-a]-quinoxaline dimaleate] were evaluated on 5-HT synthesis rates using the a-[ 14 C]methyl-L-tryptophan (a-MTrp) autoradiographic method. In the acute treatment study, TFMPP (10 mg/kg) and CGS12066B (5 mg/kg) were injected intraperitoneally 30 min before an a-MTrp injection. In an acute study TFMPP reduced overall brain 5-HT synthesis, in the dorsal and median raphe, and in almost all of their projection areas, with the exception of the parietal, sensory-motor, and frontal cortices, the accumbens nucleus, and the caudate. Acute CGS12066B treatment did not have overall significant effect, but the rates did decrease in the cell body areas of 5-HT neurons. In a 7-day treatment with TFMPP (10 mg/kg/day) or CGS12066B (5 mg/kg/day), the 5-HT synthesis rates (24 h after last dose) decrease, with both compounds, in almost all of the nerve terminal structures. TFMPP reduced the synthesis in the dorsal and median raphe, while CGS12066B reduced it only in the dorsal raphe. This data suggests that after a 7-day treatment with TFMPP and CGS12066B, the rate of 5-HT synthesis in the dorsal raphe is restored and is reduced in many projection areas. The observed effects in the 7-day treatment could also be related to actions through the postsynaptic 5-HT 1B sites and/or other 5-HT receptors since this compounds have limited selectivity. Keywords: autoradiography, CGS12066B, 5-HT1 receptor agonists, a-methyl-L-tryptophan, serotonin synthesis rate, TFMPP. Serotonin (5-HT) is involved in a wide range of physiological functions via multiple receptor subtypes. The 5-HT 1A receptors are found in the raphe nuclei of the brainstem where they function as a mediator of the feedback control of serotonergic neuronal activity. The activation of the somatodendritic 5-HT 1A receptor inhibits the serotonergic neuronal firing (Sprouse and Aghajanian 1987). It is generally accepted that this also triggers a reduction in 5-HT release and a turnover in most brain structures (Hutson et al. 1989). Recently, it was reported that the 5-HT 1A receptor agonist buspirone induces a marked reduction of 5-HT synthesis upon acute administration (Okazawa et al. 1999), and that the 5-HT 1A receptor antagonist WAY100635, generally increased the rate of 5-HT synthesis throughout the brain (Tohyama et al. 2001). The nerve terminal presynaptic 5-HT autoreceptor is of the 5-HT 1B subtype in the rat and mouse brain (Engel et al. 1986;Hamon et al. 1990 Abbreviations used: 5-HT, 5-hydroxytryptamine; 5-HIAA, 5-hydroxyindoleacetic acid; a-MTrp, a-methyl-L-tryptophan; CGS12066B, 7-trifluoromethyl-4-(4-methyl-1-piperazinyl)pyrrolo[1,2-a]-quinoxaline dimaleate; TFMPP, N-(3-trifluoromethyl) phenylpiperazine hydrochloride.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: Figmentioning

confidence: 98%

Section: Figmentioning

confidence: 99%

See 2 more Smart Citations

Effects of serotine receptors agonists, TFMPP and CGS12066B, on regional serotonin synthesis in the rat brain: an autoradiographic study

Tohyama

Yamane

Merid

et al. 2002

Journal of Neurochemistry

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“…However WKY rats are insensitive to serotonergic drugs (e.g. SSRIs and receptor agonists) in terms of activity in the EPM and OFT, immobility in the FST, or severity of gastric ulceration after stress (Chaouloff et al, 1998;Griebel et al, 1999;Lahmame and Armario, 1996;LopezRubalcava and Lucki, 2000;Pare et al, 2001;Tejani-Butt et al, 2003), suggesting serotonergic manipulation may not affect the temperamental behaviors of these rats.…”

Section: Serotonin (5-ht)mentioning

confidence: 99%