Biochemical assessment of the central 5-HT agonist activity of RU 24969 (a piperidinyl indole)

Euvrard, C.; Boissier, Jacques R.

doi:10.1016/0014-2999(80)90117-x

Cited by 87 publications

(18 citation statements)

References 18 publications

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“…The characterization of three 5-HT receptor subtypes co-expressed by IC 1 *d4 cells is obviously a first step to the analysis of their role on 5-hydroxytryptaminergic (Euvrard & Boissier 1980;Middlemiss, 1985;Engel et al, 1986;Carlson et al, 1987;Voigt et al, 1991), (ii) the presence of 5-HT2B receptors and of 5-HT during the early stages of mouse (Loric et al, 1992;Choi et al, 1994) and Drosophila (Colas et al, 1995) embryogenesis strongly suggests that 5-HT developmental functions occur, at least partly, via receptors of the 5-HT2B subtype; moreover, 5-HT2B receptors are expressed in early mouse embryonic brain (Loric et al, 1992;Choi et al, 1994), where they may have an autocrine function in the differentiation of 5-hydroxytryptaminergic neurones; (iii) the onset of the 5-HT transporter in the IC11 cell line appears to be down-regulated by 5-HT (J.M. Launay et al, unpublished observations), favouring the idea that the external 5-HT concentration is able to modulate the 5-hydroxytryptaminergic differentiation of IC1 cells; it should now be possible to examine whether 5-HT1B/lD or/and 5-HT2B receptors, already functional at day 2 of IC1 5-hydroxytryptaminergic differentiation, participate in this process.…”

Section: Discussionmentioning

confidence: 99%

Sequential onset of three 5‐HT receptors during the 5‐hydroxytryptaminergic differentiation of the murine 1C11 cell line

Kellermann

Loric

Maroteaux

et al. 1996

British J Pharmacology

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Section: Discussionmentioning

confidence: 99%

Sequential onset of three 5‐HT receptors during the 5‐hydroxytryptaminergic differentiation of the murine 1C11 cell line

Kellermann

Loric

Maroteaux

et al. 1996

British J Pharmacology

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“…For example, ligand binding studies have shown that RU-24969 has a high affinity for 5-HT, binding sites (Hunt & Oberlander, 1981). RU-24969 has been shown to decrease 5-HT turnover (Euvrard & Boissier, 1980) and decrease release of [3H]-5-HT from rat frontal cortex (Middlemiss, 1984a), indicating that the 5-HT, receptor is the 5-HT autoregulator, regulating 5-HT release. This study confirms that RU-24969 decreases 5-HT release in vitro and demonstrates that the drug also decreases extracellular 5-HT and 5-HIAA in vivo, both in anaesthetized and freely moving rats.…”

Section: Discussionmentioning

confidence: 99%

“…One of these, 5-methoxy-3(1,2,3,6-tetrahydro-4-pyridinyl)-IH-indole (RU-24969), appears from binding (Hunt & Oberlander, 1981) and behavioural (Gardner & Guy, 1983;Tricklebank, 1984, Green et al, 1984 studies to be selective for 5-HT, receptors. RU-24969 decreases 5-HT turnover as shown by a decrease in brain 5-HIAA (Euvrard & Boissier, 1980) and inhibits K+-evoked release of [3H]-5-HT from preloaded slices of the rat frontal cortex (Middlemiss, 1984a). These effects of RU-24969 support the view that the 5-HT, receptor may be the autoreceptor involved in the regulation of 5-HT release and/or turnover (Martin & Sanders-Bush, 1982;Gozlan et al, 1983).…”

Section: Introductionmentioning

confidence: 99%

The 5‐HT₁ receptor agonist RU‐24969 decreases 5‐hydroxytryptamine (5‐HT) release and metabolism in the rat frontal cortex in vitro and in vivo

Brazell¹,

Marsden²,

Nisbet³

et al. 1985

British J Pharmacology

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K+‐stimulated release of [3H]‐5‐hydroxytryptamine ([3H]‐5‐HT) from rat frontal cortex slices was decreased by the 5‐HT receptor agonists 5‐methoxy‐n1N‐dimethyltryptamine and 5‐methoxy‐3(1,2,3,6,‐tetrahydro‐4‐pyrindinyl)‐1H‐indole (RU‐24969) (1 × 10−5 M). RU‐24969 (10 mg kg−1, i.p.) decreased extracellular 5‐HT and its metabolite 5‐hydroxyindoleacetic acid measured in vivo by use of intracerebral dialysis combined with high performance liquid chromatography and electrochemical detection. The decrease in extracellular 5‐hydroxyindoleacetic acid in vivo after RU‐24969 (10 mg kg−1, i.p.) was also observed by in vivo voltammetry. The non‐selective 5‐HT antagonist metergoline prevented the RU‐24969‐induced decrease in 5‐HT release and metabolism in vivo while the 5‐HT2 receptor antagonist R‐55669 (ritanserin) did not. The results support the view that RU‐24969 stimulates a 5‐HT1 receptor that is involved in the autoregulation of 5‐HT release and metabolism.

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“…N,N-Dimethyl-5-methoxytryptamine [17] and RU24969 [9] are indole compounds structurally related to serotonin that are potent serotonin agonists as measured by binding studies in vitro and elevate serum corticosterone in rats in vivo.…”

Section: Direct Serotonin Receptor Agonistsmentioning

confidence: 99%

Serotonergic Stimulation of Pituitary-Adrenocortical Function in Rats

Fuller¹

1981

Neuroendocrinology

189

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Various pharmacologic studies have supported a stimulatory role of brain serotonin neurons in the hypothalamic regulation of pituitary-adrenocortical function in rats. The serotonin precursor L-5-hydroxytryptophan (L-5HTP), serotonin uptake inhibitors, serotonin releasers, and direct-acting serotonin agonists all elevate serum corticosterone levels in rats. The elevation of serum corticosterone by L-5HTP is stereospecific and is potentiated by monoamine oxidase inhibition or by inhibition of serotonin uptake. Elevation of serum corticosterone by direct-acting receptor agonists is not altered by uptake inhibition or by depletion of serotonin stores. The elevation of serum corticosterone by p-chloroamphetamine, a serotonin-releasing drug, is antagonized by prevention of its uptake into serotonin neurons or by prior depletion of serotonin stores. The elevation of serum corticosterone by fluoxetine (an uptake inhibitor), by 1-m-trifluoromethylphenyl)piperazine (a direct agonist), and by p-chloroamphetamine (a serotonin releaser) does not occur with close structural analogs of those compounds lacking their specific effects on serotonin neurons. Pretreatment of rats with fluoxetine potentiates the elevation of corticosterone by L-5HTP, antagonizes the elevation of corticosterone by p-chloroamphetamine (which requires active transport into the serotonin neuron in order to release serotonin) and does not alter elevation of corticosterone by quipazine or 1-m-trifluoromethylphenyl)piperazine (direct-acting serotonin agonists) or by swim stress or insulin-induced hypoglycemia. Serotonin depletion in some cases leads to enhanced responsiveness to direct-acting drugs not requiring serotonin stores. Some serotonin receptor antagonists prevent corticosterone elevation by agents that enhance serotonergic function, but the differences among antagonists with regard to their ability to block the actions of particular agonists suggests that subpopulations of serotonin receptors may be involved. Thus most in vivo studies support the postulate developed from in vitro studies that serotonin neurons stimulate the release of corticotrophin-releasing factor from the hypothalamus, leading to enhanced secretion of adrenocorticotrophin from the pituitary gland and corticosterone from the adrenal glands. The physiological role of this postulated stimulatory serotonergic pathway is unknown, but some evidence suggests it may play a part in the diurnal rhythmicity of adrenocortical function.

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Biochemical assessment of the central 5-HT agonist activity of RU 24969 (a piperidinyl indole)

Cited by 87 publications

References 18 publications

Sequential onset of three 5‐HT receptors during the 5‐hydroxytryptaminergic differentiation of the murine 1C11 cell line

Sequential onset of three 5‐HT receptors during the 5‐hydroxytryptaminergic differentiation of the murine 1C11 cell line

The 5‐HT₁ receptor agonist RU‐24969 decreases 5‐hydroxytryptamine (5‐HT) release and metabolism in the rat frontal cortex in vitro and in vivo

Serotonergic Stimulation of Pituitary-Adrenocortical Function in Rats

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Biochemical assessment of the central 5-HT agonist activity of RU 24969 (a piperidinyl indole)

Cited by 87 publications

References 18 publications

Sequential onset of three 5‐HT receptors during the 5‐hydroxytryptaminergic differentiation of the murine 1C11 cell line

Sequential onset of three 5‐HT receptors during the 5‐hydroxytryptaminergic differentiation of the murine 1C11 cell line

The 5‐HT1 receptor agonist RU‐24969 decreases 5‐hydroxytryptamine (5‐HT) release and metabolism in the rat frontal cortex in vitro and in vivo

Serotonergic Stimulation of Pituitary-Adrenocortical Function in Rats

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The 5‐HT₁ receptor agonist RU‐24969 decreases 5‐hydroxytryptamine (5‐HT) release and metabolism in the rat frontal cortex in vitro and in vivo