Date published: 2026-4-24

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Ro4368554 (CAS 478082-99-4)

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Alternate Names:
3-benzenesulfonyl-7-(4-methyl-piperazin-1-yl)-1H-indole; 7-(4-methyl-1-piperazinyl)-3-(phenylsulfonyl)-1H-Indole
CAS Number:
478082-99-4
Molecular Weight:
355.45
Molecular Formula:
C19H21N3O2S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Ro4368554 is a selective 5-HT6 receptor antagonist that binds to these receptors with a greater than 100-fold selectivity over other monoamine receptor subtypes. It has been identified as a potent agonist of the G protein-coupled receptor (GPCR) family, specifically targeting the human adenosine A2A receptor (A2AR). This receptor is involved in many physiological processes, including inflammation, cardiovascular function, and neuroprotection. In addition, activation of the A2AR has been found to have anti-tumor effects in laboratory studies.


Ro4368554 (CAS 478082-99-4) References

  1. The selective 5-HT6 receptor antagonist Ro4368554 restores memory performance in cholinergic and serotonergic models of memory deficiency in the rat.  |  Lieben, CK., et al. 2005. Neuropsychopharmacology. 30: 2169-79. PMID: 15957009
  2. Discriminative stimulus properties of the atypical antipsychotic drug clozapine in rats trained to discriminate 1.25 mg/kg clozapine vs. 5.0 mg/kg clozapine vs. vehicle.  |  Prus, AJ., et al. 2006. Behav Pharmacol. 17: 185-94. PMID: 16495726
  3. Effects of the novel 5-HT(6) receptor antagonist RO4368554 in rat models for cognition and sensorimotor gating.  |  Schreiber, R., et al. 2007. Eur Neuropsychopharmacol. 17: 277-88. PMID: 16989988
  4. Increased expression of 5-HT6 receptors in the nucleus accumbens blocks the rewarding but not psychomotor activating properties of cocaine.  |  Ferguson, SM., et al. 2008. Biol Psychiatry. 63: 207-13. PMID: 17631868
  5. 5-HT6 receptor antagonist reversal of emotional learning and prepulse inhibition deficits induced by apomorphine or scopolamine.  |  Mitchell, ES. and Neumaier, JF. 2008. Pharmacol Biochem Behav. 88: 291-8. PMID: 17920665
  6. Selective 5HT2A and 5HT6 receptor antagonists promote sleep in rats.  |  Morairty, SR., et al. 2008. Sleep. 31: 34-44. PMID: 18220076
  7. Adaptations in 5-HT receptor expression and function: implications for treatment of cognitive impairment in aging.  |  Mitchell, ES., et al. 2009. J Neurosci Res. 87: 2803-11. PMID: 19396878
  8. Effects of the 5-HT₆ receptor antagonists SB-399885 and RO-4368554 and of the 5-HT(2A) receptor antagonist EMD 281014 on sleep and wakefulness in the rat during both phases of the light-dark cycle.  |  Monti, JM. and Jantos, H. 2011. Behav Brain Res. 216: 381-8. PMID: 20732355
  9. Effects of 5-HT6 antagonists, Ro-4368554 and SB-258585, in tests used for the detection of cognitive enhancement and antipsychotic-like activity.  |  Gravius, A., et al. 2011. Behav Pharmacol. 22: 122-35. PMID: 21301322
  10. Procognitive profiling of a serotonin 5-HT6 receptor antagonist in a complex model system in rats: A novel translational approach for clinical prediction.  |  Gyertyán, I., et al. 2020. Brain Res Bull. 165: 238-245. PMID: 33086133

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Ro4368554, 5 mg

sc-253435
5 mg
$200.00