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Chemical Compound Review:

CHEMBL14563 6-chloro-5-methyl-N-[6-(2- methylpyridin-3...

Synonyms: AC1MUPO0, SureCN507945, CHEBI:114131, SB-242084, PDSP1_001569, ...

Fletcher, P.J. et al., Hayashi, A. et al., Quinn, L.P. et al., Kimura, Y. et al., Hayashi, A. et al., et al.

Quinn, Stean, Trail, Duxon, Stratton, Billinton, Upton, Kimura, Naitou, Wanibuchi, Yamaguchi, Hayashi, Suzuki, Sasamata, Miyata, Fletcher, Sinyard, Higgins, Hayashi, Sonoda, Kimura, Takasu, Suzuki, Sasamata, Miyata,

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Disease relevance of SB242084

YM348- or RO 60-0175-induced hyperthermia was significantly attenuated by the non-selective 5-HT(2)-receptor antagonist methysergide and the selective 5-HT(2C)-receptor antagonist SB242084, but not by the selective 5-HT(2A)-receptor antagonist MDL100907. mCPP-induced hyperthermia was significantly attenuated by methysergide, SB242084 and MDL100907 [1].

Psychiatry related information on SB242084

The effects of the 5-HT(2C) receptor antagonist SB242084 on locomotor activity induced by selective, or mixed, indirect serotonergic and dopaminergic agonists [2].

High impact information on SB242084

The selective 5-HT2C receptor antagonist SB242084 [(6-chloro-5-methyl-1-[6-(2-methylpyridin-3-yloxy) pyridin-3-yl carbamoyl] indoline)] (0.03 to 1 mg/kg intraperitoneally) was administered 30 minutes before YM348 treatment [3].
MATERIALS AND METHODS: Male Sprague-Dawley rats were treated in the presence or absence of SB242084 with releasers/reuptake inhibitors of DA (amphetamine and methylphenidate), 5-HT (fenfluramine and citalopram), or both 5-HT and DA (MDMA and cocaine) [2].
The increasing effect of YM348 on body temperature and calorie expenditure was inhibited by SB242084 [4].

Chemical compound and disease context of SB242084

Data were obtained from rats administered with mCPP (reversal with SB242084), 8-OH-DPAT (reversal with WAY100635), amphetamine (reversal with haloperidol) and angiotensin, with the focus on locomotor activity, feeding and drinking behaviours [5].

Biological context of SB242084

This effect of YM348 on food intake was inhibited by SB242084, a selective 5-HT2C receptor antagonist [4].

Gene context of SB242084

A 5-HT2C receptor antagonist, SB242084, did not block the effect of DOM [6].

References

Thermogenic effect of YM348, a novel 5-HT2C-receptor agonist, in rats. Hayashi, A., Suzuki, M., Sasamata, M., Miyata, K. J. Pharm. Pharmacol. (2004) [Pubmed]
The effects of the 5-HT(2C) receptor antagonist SB242084 on locomotor activity induced by selective, or mixed, indirect serotonergic and dopaminergic agonists. Fletcher, P.J., Sinyard, J., Higgins, G.A. Psychopharmacology (Berl.) (2006) [Pubmed]
Characterization of intracavernous pressure increase induced by Ym348, a novel 5-HT2C receptor agonist, in anesthetized rats. Kimura, Y., Naitou, Y., Wanibuchi, F., Yamaguchi, T. J. Urol. (2006) [Pubmed]
Antiobesity effect of YM348, a novel 5-HT2C receptor agonist, in Zucker rats. Hayashi, A., Sonoda, R., Kimura, Y., Takasu, T., Suzuki, M., Sasamata, M., Miyata, K. Brain Res. (2004) [Pubmed]
LABORAS: Initial pharmacological validation of a system allowing continuous monitoring of laboratory rodent behaviour. Quinn, L.P., Stean, T.O., Trail, B., Duxon, M.S., Stratton, S.C., Billinton, A., Upton, N. J. Neurosci. Methods (2003) [Pubmed]
Characterization of a novel effect of serotonin 5-HT1A and 5-HT2A receptors: increasing cGMP levels in rat frontal cortex. Regina, M.J., Winter, J.C., Rabin, R.A. Neuropharmacology (2003) [Pubmed]

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