Evidence that hypophagia induced by d-fenfluramine and d-norfenfluramine in the rat is mediated by 5-HT2C receptors

@article{Vickers2001EvidenceTH,
  title={Evidence that hypophagia induced by d-fenfluramine and d-norfenfluramine in the rat is mediated by 5-HT2C receptors},
  author={S. Vickers and C. Dourish and G. Kennett},
  journal={Neuropharmacology},
  year={2001},
  volume={41},
  pages={200-209}
}
The present series of studies is the first to investigate the pharmacological mechanisms underlying d-fenfluramine- and d-norfenfluramine-induced hypophagia in the rat using highly selective serotonin 5-HT2 receptor antagonists. Administration of d-fenfluramine, and its major metabolite d-norfenfluramine, suppresses food intake in animals. Both compounds stimulate the release of serotonin and are potent inhibitors of the re-uptake of 5-HT into nerve terminals. In addition, d-norfenfluramine… Expand
Reduced hypophagic effects of d-fenfluramine and the 5-HT2C receptor agonist mCPP in 5-HT1B receptor knockout mice
TLDR
The evidence suggests that an adaptive change in5-HT2C receptor function occurs in 5-HT1B receptor KO mice and contributes to their reduced response to d-fenfluramine. Expand
Parabrachial infusion of d-fenfluramine reduces food intake Blockade by the 5-HT1B antagonist SB-216641
TLDR
The data strongly suggest that directly or indirectly activating 5-HT(1B) receptors in the LPBN inhibits feeding and implicates this pontine region in the serotonergic regulation of eating and satiation. Expand
3,4-N-Methlenedioxymethamphetamine-Induced Hypophagia is Maintained in 5-HT1B Receptor Knockout Mice, but Suppressed by the 5-HT2C Receptor Antagonist RS102221
TLDR
These findings provide the first evidence that the in activation of 5-HT2C receptors may reduce hypophagia and motor response to MDMA, while a genetic deficit or pharmacological inactivation of5-HT1B receptors was insufficient to alter the feeding response to ecstasy. Expand
Effects of fenfluramine on free-operant timing behaviour: evidence for involvement of 5-HT2A receptors
TLDR
The results suggest that fenfluramine affects temporal differentiation via the release of endogenous 5-HT which acts mainly on postsynaptic 5- HT2A receptors. Expand
Fluvoxamine, a selective serotonin reuptake inhibitor, and 5-HT2C receptor inactivation induce appetite-suppressing effects in mice via 5-HT1B receptors.
TLDR
It is suggested that fluvoxamine and inactivation of 5-HT2C receptors exert feeding suppression through activation of5-HT1B receptors, and that 4C receptors up-regulates hypothalamic POMC and CART gene expression and down-regulate hypothalamic orexin gene expression in mice. Expand
(+)-Fenfluramine and Its Major Metabolite, (+)-Norfenfluramine, Are Potent Substrates for Norepinephrine Transporters
TLDR
Administration of fenfluramines can increase synaptic levels of 5-HT, NE, and DA in the cortex, and (+)-norfenfluramine likely contributes to these effects. Expand
Medial parabrachial nucleus neurons modulate d-fenfluramine-induced anorexia through 5HT2C receptors
TLDR
Results from the present study are consistent with the hypothesis that medial PBN neurons mediate anorexia through 5HT2C receptors. Expand
Serotonin 2C receptor agonists and the behavioural satiety sequence in mice
TLDR
The data suggest that Ro 60-0175- and mCPP-induced hypophagia in mice are mediated via activation of 5-HT(2C) receptors and that stimulation of 6-chloro-5-fluoro-indol-l-yl)-l-methylethylamine hydrochloride plays only a minor role in mCP piperazine- induced hypophgia. Expand
Serotonergic and histaminergic mechanisms involved in intralipid drinking?
TLDR
To examine the possible contribution of serotonin (5-HT) and histamine (H) receptor blockade in antipsychotic-associated hyperphagia, rats were trained to drink a palatable, high-calorie fat emulsion and tested following pretreatment with mepyramine, metergoline, cyproheptadine and an SB 242084-mepyramine combination. Expand
Investigating interactions between phentermine, dexfenfluramine, and 5-HT2C agonists, on food intake in the rat
TLDR
Dexfenfluramine-phentermine synergy in the rat is caused by a pharmacokinetic interaction, resulting in increased central concentrations of phentermine. Expand
...
1
2
3
4
5
...

References

SHOWING 1-10 OF 40 REFERENCES
Reduced satiating effect of d-fenfluramine in serotonin 5-HT2C receptor mutant mice
TLDR
A role for the 5-HT2C receptor in mediating d-fenfluramine-induced satiety is demonstrated and is demonstrated to be a potent inhibitor of the re-uptake of5-HT into nerve terminals and a facilitator of behavioural satiety in mutant mice. Expand
5-HT and carbohydrate suppression: Effects of 5-HT antagonists on the action of d-fenfluramine and DOI
TLDR
The suppressive effect of these two 5-HT drugs on total and Polycose intake appears to be mediated, respectively, by 5-ht1B/5-HT1C receptors (d-fenfluramine) and 5- HT2 receptors (DOI). Expand
Role of 5-HT receptors in the effect of d-fenfluramine on feeding patterns in the rat.
TLDR
The results suggest that 5- HT1 receptors, possibly of the 5-HT1B type, are involved in the ability of d-fenfluramine to cause satiety in freely feeding rats. Expand
Absence of Fenfluramine-Induced Anorexia and Reduced c-fos Induction in the Hypothalamus and Central Amygdaloid Complex of Serotonin 1B Receptor Knock-Out Mice
TLDR
It is demonstrated that stimulation of 5-HT1B receptors is required for fenfluramine-induced anorexia and a role for the PVN, CeA, and BNST in mediating this effect is suggested. Expand
Stimulation of 5-HT1B receptors causes hypothermia in the guinea pig.
TLDR
The present study shows that the hypothermic response to SKF-99101H is dose-dependently blocked by SB-224289G, which is the first compound to be described which is more than 60 fold selective for the 5-HT1B receptor over the 4-chloro-5-propoxyindole hemifumarate receptor. Expand
Studies on the role of 5-HT2C and 5-HT2B receptors in regulating generalised seizure threshold in rodents.
TLDR
The results indicate that the observed anticonvulsant effects of mCPP are likely to be mediated by activation of 5-HT2C receptors, suggesting that in normal adult animals this receptor subtype may usually be subjected to only a low level of5-hydroxytryptamine tone. Expand
Studies on the role of serotonin receptor subtypes in the effect of sibutramine in various feeding paradigms in rats
TLDR
5‐HT1 and 5‐HT2 receptor subtypes do not play an important role in the hypophagic effect of sibutramine, at least in the first 2 h after injection, and the results suggest that, with the possible exception of a partial involvement of 5‐ HT2B/2C receptors in sibUTramine's hypophagia in food‐deprived rats. Expand
Electrophysiological, biochemical, neurohormonal and behavioural studies with WAY-100635, a potent, selective and silent 5-HT1A receptor antagonist
TLDR
In vitro electrophysiological studies demonstrated that WAY-100635 had no 5-HT1A receptor agonist actions, but dose-dependently blocked the effects of agonists at both the postsynaptic5-HT 1A receptor in the CA1 region of the hippocampus, and the somatodendritic 5-ht1A receptors located on dorsal raphe 5- HT neurones. Expand
Anxiolytic-like actions of BW 723C86 in the rat Vogel conflict test are 5-HT2B receptor mediated
TLDR
The 5-HT2B receptor agonist, BW 723C86, increased the number of punishments accepted in a rat Vogel drinking conflict paradigm over 3 min, as did the benzodiazepine anxiolytics, chlordiazepoxide (2.5-10 mg/kg p.o.p) and alprazolam (0.3-3mg/kg i.p). Expand
(1-(2,5-dimethoxy-4 iodophenyl)-2-aminopropane)-induced head-twitches in the rat are mediated by 5-hydroxytryptamine (5-HT) 2A receptors: modulation by novel 5-HT2A/2C antagonists, D1 antagonists and 5-HT1A agonists.
TLDR
It is demonstrated that 5-HT2A receptors mediate HTW in rats and that both D1 and D2 receptors as well as (postsynaptic) 5- HT1A receptors play a role in their expression. Expand
...
1
2
3
4
...