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Chemical Compound Review:

Tocris-0989 1-(4-amino-5-chloro-2- methoxy-phenyl)-3-(1...

Synonyms: CHEMBL85251, SureCN549019, BPBio1_000441, AC1L4DLZ, RS-67333, ...

Marchetti, E. et al., Marchetti, E. et al., Lamirault, L. et al., Fontana, D.J. et al., Eglen, R.M. et al., et al.

Lamirault, Simon, Marchetti, Dumuis, Bockaert, Soumireu-Mourat, Roman,

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High impact information on Tocris-0989

The modulating role of the 5-HT4 receptors was studied by using a potent, 5-HT4 partial agonist RS 67333 [1-(4-amino-5-chloro-2-methoxyphenyl)-3-(1-n-butyl-4-piperidinyl)-1-propanone] and a selective 5-HT4 receptor antagonist RS 67532 [1-(4-amino-5-chloro-2-(3,5-dimethoxybenzyloxyphenyl)-5-(1-piperidinyl)-1-propanone] [1].
In the present study, the effects of two potent and selective 5-HT(4) agonists, RS 17017 [1-(4-amino-5-chloro-2-methoxyphenyl)-5- (piperidin-1-yl)-1-pentanone hydrochloride] and RS 67333 [1(4-amino-5-chloro-2-methoxyphenyl)-3- (1-n-butyl-4-piperidinyl)-1-propanone], were studied in an olfactory associative discrimination task [2].
Pharmacological characterization of two novel and potent 5-HT4 receptor agonists, RS 67333 and RS 67506, in vitro and in vivo [3].
However, RS 67333 and RS 67506 did exhibit affinities for the sigma 1 (pKi = 8.9 and 7.9, respectively) and sigma 2 (pKi = 8.0 and 7.3, respectively) binding sites [3].
BIMU 1 and RS 67333, two 5-HT4 receptor agonists, modulate spontaneous alternation deficits induced by scopolamine in the mouse [4].

Associations of Tocris-0989 with other chemical compounds

In separate locomotor studies, RS 67532 reduced activity at 1 and 10 mg/kg, i.p., although no effect was seen with RS 67333 or RS 67506 (0.01-10 mg/kg, i.p.). These data suggest that RS 67333 reversed the cognitive deficit induced by atropine and support a role of 5-HT4 receptors in rat spatial learning and memory [5].
This facilitatory effect of 5-HT was partially mimicked by both selective 5-HT3 (2-methyl-5-HT) and 5-HT4 (RS 67333 and 5-methoxytryptamine) agonists [6].

Gene context of Tocris-0989

Enhancement of place and object recognition memory in young adult and old rats by RS 67333, a partial agonist of 5-HT4 receptors [7].
The present study was designed to investigate whether a combination of a new acetylcholinesterase inhibitor we have synthesized, galanthaminium bromide, and an agonist of 5-hydroxytryptamine(4) receptors, RS 67333, at doses ineffective alone, improves performance in tasks involving place and object recognition memory [8].

References

Modulation of memory processes and cellular excitability in the dentate gyrus of freely moving rats by a 5-HT4 receptors partial agonist, and an antagonist. Marchetti, E., Chaillan, F.A., Dumuis, A., Bockaert, J., Soumireu-Mourat, B., Roman, F.S. Neuropharmacology (2004) [Pubmed]
Differential modulation of the 5-HT(4) receptor agonists and antagonist on rat learning and memory. Marchetti, E., Dumuis, A., Bockaert, J., Soumireu-Mourat, B., Roman, F.S. Neuropharmacology (2000) [Pubmed]
Pharmacological characterization of two novel and potent 5-HT4 receptor agonists, RS 67333 and RS 67506, in vitro and in vivo. Eglen, R.M., Bonhaus, D.W., Johnson, L.G., Leung, E., Clark, R.D. Br. J. Pharmacol. (1995) [Pubmed]
BIMU 1 and RS 67333, two 5-HT4 receptor agonists, modulate spontaneous alternation deficits induced by scopolamine in the mouse. Lelong, V., Lhonneur, L., Dauphin, F., Boulouard, M. Naunyn Schmiedebergs Arch. Pharmacol. (2003) [Pubmed]
The effects of novel, selective 5-hydroxytryptamine (5-HT)4 receptor ligands in rat spatial navigation. Fontana, D.J., Daniels, S.E., Wong, E.H., Clark, R.D., Eglen, R.M. Neuropharmacology (1997) [Pubmed]
The effects of 5-HT on cholinergic contraction in human airways in vitro. Dupont, L.J., Pype, J.L., Demedts, M.G., De Leyn, P., Deneffe, G., Verleden, G.M. Eur. Respir. J. (1999) [Pubmed]
Enhancement of place and object recognition memory in young adult and old rats by RS 67333, a partial agonist of 5-HT4 receptors. Lamirault, L., Simon, H. Neuropharmacology (2001) [Pubmed]
Combined treatment with galanthaminium bromide, a new cholinesterase inhibitor, and RS 67333, a partial agonist of 5-HT4 receptors, enhances place and object recognition in young adult and old rats. Lamirault, L., Guillou, C., Thal, C., Simon, H. Prog. Neuropsychopharmacol. Biol. Psychiatry (2003) [Pubmed]

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