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Chemical Compound Review

CHEMBL2331803     but-2-enedioic acid; (2S)-1-(6-chloro-5...

Synonyms: SureCN8959555, LS-183389, AC1O64DP, Ro 60-0175, 169675-09-6
 
 
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Disease relevance of Ro 60-0175

  • In a final series of studies to examine the cataleptogenic properties of Ro 60-0175, very mild indices of catalepsy were observed at the 3 mg/kg dose only [1].
  • Interestingly, DOI (10 - 1000 microg kg(-1), i.v.) induced only slight, dose-unrelated, tachycardic responses, whilst the 5-HT(2C) agonist, Ro 60-0175 (10 - 1000 microg kg(-1), i.v.), produced a slight tachycardia only at 300 and 1000 microg kg(-1) [2].
  • 5. These data suggest tolerance does not develop to the effects of d-fenfluramine, mCPP and Ro 60-0175 on rat body weight gain [3].
 

Psychiatry related information on Ro 60-0175

 

High impact information on Ro 60-0175

  • However, the combination of Ro 60-0175 with CP-94,253 induced a substantial increase in activity in 5-HT2C KO mice, an effect comparable to mCPP-induced hyperactivity [4].
  • Injection of Ro 60-0175 (5 mg/kg s.c.) produced a maximum increase in plasma levels of adrenocorticotrophic hormone, oxytocin, and prolactin at 15 min postinjection and a maximum increase in plasma corticosterone levels at 60 min postinjection [8].
  • Furthermore, increasing doses (from 1.25 to 40 mg/kg, IP) of S 21517 and S 21540, the two main metabolites of agomelatine, did not affect the penile erections induced by mCPP and Ro 60-0175 [9].
  • The NMDA-induced cyclic GMP elevation also was potently inhibited by the selective 5-HT(2C) agonist RO 60-0175 and by the antidepressant trazodone, both added at 1 microM, in an SB 242084-sensitive manner [10].
  • Alpha2-AR antagonist properties were revealed in vivo by blockade of UK-14,304-induced antinociception, while antagonist actions at 5-HT2C receptors were demonstrated by blockade of Ro 60 0175-induced penile erections and discriminative stimulus properties [11].
 

Biological context of Ro 60-0175

 

Anatomical context of Ro 60-0175

  • Stimulation of 5-HT2C receptors by RO 60-0175 (1 mg/kg, i.p.) significantly decreased DA release in the nucleus accumbens by 26.1+/-4% (below baseline) 60 min after injection [14].
  • Moreover, RO 60-0175 (80-320 microg/kg, i.v.) dose-dependently decreased the basal firing rate of DA neurons in the ventral tegmental area (VTA), reaching its maximal inhibitory effect (53.9+/-15%, below baseline) after the dose of 320 microg/kg [15].
 

Associations of Ro 60-0175 with other chemical compounds

  • Injection of the 5-HT2C receptor agonist RO 60-0175 (80-320% microg/kg, i.v.) dose-dependently decreased the basal firing of DA neurons in the VTA but not in the SNc [14].
  • 8-OH-DPAT-induced spontaneous tail-flicks in the rat are facilitated by the selective serotonin (5-HT)2C agonist, RO 60-0175: blockade of its actions by the novel 5-HT2C receptor antagonist SB 206,553 [16].
  • This response was potentiated by the selective 5-HT2C receptor agonist, RO 60-0175 ((S)-2-(6-chloro-5-fluoroindol-1-yl)-1-methylethylamine) fumarate) (0.16 mg/kg, s.c.), the action of which was abolished by the novel 5-HT2C antagonist, SB 206,553 (5 methyl-1-(3-pyridil-carbamoyl)-1,2,3,5-tetrahydropyrrolo[2,3 -f]indole) (0.16 mg/kg, s.c [16].
  • Behavioural satiety sequence (BSS) and food intake measurements were taken, comparing the selective 5-HT(2C) receptor agonist (S)-2-(6-chloro-5-fluoro-indol-l-yl)-l-methylethylamine hydrochloride (Ro 60-0175; 1.0, 3.0 and 10.0 mg/kg) and D-fenfluramine (3.0 mg/kg) [12].
 

Gene context of Ro 60-0175

  • In vivo, SB 206553 (1-10 mg/kg) elicited a dose-dependent and clear-cut increase in accumbal and striatal DA release compared with SB 242084 (1-10 mg/kg), and the 5-HT2C agonist S-2-(6-chloro-5-fluoroindol-1-yl)-1-methylethylamine hydrochloride (Ro-60-0175) (0.3-3 mg/kg) inhibited DA release [17].
  • In addition, lower doses of mianserin (2.5 mg/kg i.p.) and amitriptyline (5 mg/kg i.p.) blocked the inhibitory action of RO 60-0175 (1 mg/kg i.p.), a selective 5-HT2C receptor agonist, on DA release [18].
 

Analytical, diagnostic and therapeutic context of Ro 60-0175

  • Effects of RO 60 0175, a 5-HT(2C) receptor agonist, in three animal models of anxiety [6].
  • Currently, a new generation of 5-HT(2C) selective agonists have been developed (including Ro 60-0175, Org 12962, VER-3323, BVT-933 and YM348) and at least one, ADP356, is currently undergoing clinical trials [19].

References

  1. Studies to investigate the role of 5-HT(2C) receptors on cocaine- and food-maintained behavior. Grottick, A.J., Fletcher, P.J., Higgins, G.A. J. Pharmacol. Exp. Ther. (2000) [Pubmed]
  2. The atypical 5-HT2 receptor mediating tachycardia in pithed rats: pharmacological correlation with the 5-HT2A receptor subtype. Centurión, D., Ortiz, M.I., Saxena, P.R., Villalón, C.M. Br. J. Pharmacol. (2002) [Pubmed]
  3. Comparative effects of continuous infusion of mCPP, Ro 60-0175 and d-fenfluramine on food intake, water intake, body weight and locomotor activity in rats. Vickers, S.P., Benwell, K.R., Porter, R.H., Bickerdike, M.J., Kennett, G.A., Dourish, C.T. Br. J. Pharmacol. (2000) [Pubmed]
  4. mCPP-induced hyperactivity in 5-HT2C receptor mutant mice is mediated by activation of multiple 5-HT receptor subtypes. Dalton, G.L., Lee, M.D., Kennett, G.A., Dourish, C.T., Clifton, P.G. Neuropharmacology (2004) [Pubmed]
  5. Similarities in the action of Ro 60-0175, a 5-HT2C receptor agonist and d-fenfluramine on feeding patterns in the rat. Clifton, P.G., Lee, M.D., Dourish, C.T. Psychopharmacology (Berl.) (2000) [Pubmed]
  6. Effects of RO 60 0175, a 5-HT(2C) receptor agonist, in three animal models of anxiety. Kennett, G., Lightowler, S., Trail, B., Bright, F., Bromidge, S. Eur. J. Pharmacol. (2000) [Pubmed]
  7. The role of 5-HT2C receptors in affective disorders. Jenck, F., Bös, M., Wichmann, J., Stadler, H., Martin, J.R., Moreau, J.L. Expert opinion on investigational drugs. (1998) [Pubmed]
  8. Neuroendocrine evidence that (S)-2-(chloro-5-fluoro-indol- l-yl)-1-methylethylamine fumarate (Ro 60-0175) is not a selective 5-hydroxytryptamine(2C) receptor agonist. Damjanoska, K.J., Muma, N.A., Zhang, Y., D'Souza, D.N., Garcia, F., Carrasco, G.A., Kindel, G.H., Haskins, K.A., Shankaran, M., Petersen, B.R., Van De Kar, L.D. J. Pharmacol. Exp. Ther. (2003) [Pubmed]
  9. Agomelatine(S 20098) antagonizes the penile erections induced by the stimulation of 5-HT2C receptors in Wistar rats. Chagraoui, A., Protais, P., Filloux, T., Mocaër, E. Psychopharmacology (Berl.) (2003) [Pubmed]
  10. Serotonin inhibition of the NMDA receptor/nitric oxide/cyclic GMP pathway in human neocortex slices: involvement of 5-HT(2C) and 5-HT(1A) receptors. Maura, G., Marcoli, M., Pepicelli, O., Rosu, C., Viola, C., Raiteri, M. Br. J. Pharmacol. (2000) [Pubmed]
  11. Mirtazapine enhances frontocortical dopaminergic and corticolimbic adrenergic, but not serotonergic, transmission by blockade of alpha2-adrenergic and serotonin2C receptors: a comparison with citalopram. Millan, M.J., Gobert, A., Rivet, J.M., Adhumeau-Auclair, A., Cussac, D., Newman-Tancredi, A., Dekeyne, A., Nicolas, J.P., Lejeune, F. Eur. J. Neurosci. (2000) [Pubmed]
  12. Serotonin 2C receptor agonists and the behavioural satiety sequence in mice. Hewitt, K.N., Lee, M.D., Dourish, C.T., Clifton, P.G. Pharmacol. Biochem. Behav. (2002) [Pubmed]
  13. 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]
  14. SB 242084, a selective serotonin2C receptor antagonist, increases dopaminergic transmission in the mesolimbic system. Di Matteo, V., Di Giovanni, G., Di Mascio, M., Esposito, E. Neuropharmacology (1999) [Pubmed]
  15. Biochemical and electrophysiological evidence that RO 60-0175 inhibits mesolimbic dopaminergic function through serotonin(2C) receptors. Di Matteo, V., Di Giovanni, G., Di Mascio, M., Esposito, E. Brain Res. (2000) [Pubmed]
  16. 8-OH-DPAT-induced spontaneous tail-flicks in the rat are facilitated by the selective serotonin (5-HT)2C agonist, RO 60-0175: blockade of its actions by the novel 5-HT2C receptor antagonist SB 206,553. Millan, M.J., Girardon, S., Bervoets, K. Neuropharmacology (1997) [Pubmed]
  17. Constitutive activity of the serotonin2C receptor inhibits in vivo dopamine release in the rat striatum and nucleus accumbens. De Deurwaerdère, P., Navailles, S., Berg, K.A., Clarke, W.P., Spampinato, U. J. Neurosci. (2004) [Pubmed]
  18. Acute administration of amitriptyline and mianserin increases dopamine release in the rat nucleus accumbens: possible involvement of serotonin2C receptors. Di Matteo, V., Di Mascio, M., Di Giovanni, G., Esposito, E. Psychopharmacology (Berl.) (2000) [Pubmed]
  19. Serotonin (5-HT) drugs: effects on appetite expression and use for the treatment of obesity. Halford, J.C., Harrold, J.A., Lawton, C.L., Blundell, J.E. Current drug targets. (2005) [Pubmed]
 
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