Antiobesity effect of YM348, a novel 5-HT2C receptor agonist, in Zucker rats

@article{Hayashi2004AntiobesityEO,
  title={Antiobesity effect of YM348, a novel 5-HT2C receptor agonist, in Zucker rats},
  author={Aska Hayashi and Rie Sonoda and Yasuharu Kimura and Toshiyuki Takasu and Masanori Suzuki and Masao Sasamata and Keiji Miyata},
  journal={Brain Research},
  year={2004},
  volume={1011},
  pages={221-227}
}

Agonist diversity in 5-HT2C receptor-mediated weight control in rats

Together, the difference between compounds in their hypophagic effects and the similarity in their hyperthermic effects suggest a diversity in agonists in 5-HT2C receptor-mediated weight control in rats.

Serotonin 1B and 2C receptor interactions in the modulation of feeding behaviour in the mouse

5-HT2C-R and 5-HT1B-R activation are each sufficient to induce a hypophagic response, however, concurrent 5- HT2c-R inactivation can potentiate the hypophotic response to 5-ht1b-Ractivation, consistent with an inhibitory role for the 5-hydroxytryptamine-based response in behaviour mediated by the activation of other 4-HT receptors.

Lorcaserin, a Novel Selective Human 5-Hydroxytryptamine2C Agonist: in Vitro and in Vivo Pharmacological Characterization

Data demonstrate lorcaserin to be a potent, selective, and efficacious agonist of the 5-HT2C receptor, with potential for the treatment of obesity.

Antidepressant-like effects of the novel, selective, 5-HT2C receptor agonist WAY-163909 in rodents

The results demonstrate that the novel 5-HT2C receptor agonist WAY-163909 produces rapid onset antidepressant-like effects in animal models and may be a novel treatment for depression.

Pharmacological profile of the 5-HT(2C) receptor agonist WAY-163909; therapeutic potential in multiple indications.

5-HT(2C) receptor selective agonist WAY-163909 was found to have robust dose-dependent effects in animal models of obesity, psychotic-like behavior or depression, consistent with a potential therapeutic utility in obesity, schizophrenia and depression.

5-HT(2C) receptor agonists and the control of appetite.

Lorcaserin, a selective 5-HT(2C) receptor agonist, is a novel anti-obesity agent that reduces both energy intake and body weight and remains to be characterised as does its behavioural specificity.

Serotonin 5-ht2c receptor agonists: potential for the treatment of obesity.

  • K. Miller
  • Medicine, Biology
    Molecular interventions
  • 2005
Development of highly selective 5-HT(2C) agonists may recapitulate the clinical anti-obesity properties observed with fenfluramine while avoiding the significant cardiovascular and pulmonary side effects.

References

SHOWING 1-10 OF 27 REFERENCES

Similarities in the action of Ro 60-0175, a 5-HT2C receptor agonist, and d-fenfluramine on feeding patterns in the rat

The hypothesis that activation of 5-HT2C receptors is a critical aspect of the hypophagic action of d-fenfluramine is supported and may prove to be a useful target in the development of clinically effective drugs for the treatment of obesity.

Chronic treatment with meta-chlorophenylpiperazine (m-CPP) alters behavioral and cerebral metabolic responses to the serotonin agonists m-CPP and quipazine but not 8-hydroxy-2(di-N-propylamino)tetralin

It is suggested that hypolocomotion and the serotonin syndrome are mediated by different 5-HT receptor subtypes, and that chronic m-CPP administration produces functional down-regulation of 5- HT1B/1C but not of 5 -HT1A-coupled mechanisms.

Evidence thatm-chlorophenylpiperazine-induced hyperthermia in rats is mediated by stimulation of 5-HT2C receptors

Findings suggest thatm-CPP-induced hyperthermia in rats is mediated by selective stimulation of 5-HT2C receptors.

Evidence that hypophagia induced bymCPP and TFMPP requires 5-HT1C and 5-HT1B receptors; hypophagia induced by RU 24969 only requires 5-HT1B receptors

The results suggest that RU 24969-induced hypophagia depends on 5-HT1B receptors but not on 5,HT1C receptors, whilemCPP (and TFMPP)-induced hypolocomotion may depend on both receptors.

Evidence that mCPP may have behavioural effects mediated by central 5‐HT1C receptors

As mianserin, cyproheptadine and mesulergine in the absence of mCPP did not increase locomotion but increased the number of feeding scores, the activation of 5‐HT1C‐receptors may be of physiological importance in the control of appetite.

Hyperthermia induced by m-CPP in the rat and its modification by antidepressant treatments

In studies investigating the modification of the response by antidepressant treatments both acute (3 day) and chronic (22 day) administration of the MAO inhibitor clorgyline, as well as the tricyclics clomipramine and imipramines, attenuated the hyperthermic response to m-CPP.