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Chemical Compound Review:

Tocris-1242 N-[3-(2-dimethylaminoethoxy)- 4-methoxy...

Synonyms: AC1MMVTS, CHEMBL20963, SureCN2360553, S8942_SIGMA, BPBio1_000134, ...

Schlicker, E. et al., Harsing, L.G. et al., Mancilla-Diaz, J.M. et al., Price, G.W. et al., Simansky, K.J. et al.

Harsing, Prauda, Barkoczy, Matyus, Juranyi, Simansky, Nicklous,

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High impact information on Tocris-1242

In conclusion, SB-216641 behaves as a preferential antagonist at native human 5-HT1B receptors and BRL-15572 as a preferential antagonist at native human 5-HT1D receptors [1].
Effects of selective h5-HT1B (SB-216641) and h5-HT1D (BRL-15572) receptor ligands on guinea-pig and human 5-HT auto- and heteroreceptors [1].
In human atrial appendages, the electrically evoked tritium overflow was inhibited by 5-HT in a manner susceptible to antagonism by BRL-15572 (300 nM; 23 times Ki at h5-HT1D receptors) but not by SB-216641 (30 nM; 30 times Ki at h5-HT1B receptors) [1].
In human cerebral cortex slices SB-216641 (0.1 microM) also facilitated, and BRL-15572 (2 microM) again failed to affect, the electrically evoked tritium overflow [1].
In receptor binding studies on human receptors expressed in CHO cells, SB-216641 has high affinity (pKi = 9.0) for h5-HT1B receptors and has 25-fold lower affinity at h5-HT1D receptors [2].

Biological context of Tocris-1242

Parabrachial infusion of D-fenfluramine reduces food intake. Blockade by the 5-HT(1B) antagonist SB-216641 [3].
This effect of 5-CT on [3H]5-HT overflow was antagonized by the 5-HT7 receptor antagonist SB-258719 (10 microM) and the 5-HT(1B/1D) antagonist SB-216641 (1 microM), the IC50 values for 5-CT in the presence of SB-258719 and SB-216641 were 94.23 +/- 4.84 and 47.81 +/- 4.66 nM [4].

Anatomical context of Tocris-1242

Blockade of 5-HT1A or 5-HT1B receptors in the paraventricular nucleus was effected by WAY 100635 (2 microg) or SB-216641 (2 microg) pretreatment; ten minutes later, 5-HT (2 microg) was applied into the same nucleus, then food intake and meal patterns were measured in a 30-minute period [5].

Associations of Tocris-1242 with other chemical compounds

The antagonist effect of SB-258719 (10 microM) on 5-CT-evoked [3H]5-HT overflow inhibition was also determined in the presence of 1 microM SB-216641 or 1 microM SB-216641 and 10 microM WAY-100635, and additive interactions were found between the antagonists of 5-HT7 and 5-HT1 receptor subtypes [4].

References

Effects of selective h5-HT1B (SB-216641) and h5-HT1D (BRL-15572) receptor ligands on guinea-pig and human 5-HT auto- and heteroreceptors. Schlicker, E., Fink, K., Molderings, G.J., Price, G.W., Duckworth, M., Gaster, L., Middlemiss, D.N., Zentner, J., Likungu, J., Göthert, M. Naunyn Schmiedebergs Arch. Pharmacol. (1997) [Pubmed]
SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors. Price, G.W., Burton, M.J., Collin, L.J., Duckworth, M., Gaster, L., Göthert, M., Jones, B.J., Roberts, C., Watson, J.M., Middlemiss, D.N. Naunyn Schmiedebergs Arch. Pharmacol. (1997) [Pubmed]
Parabrachial infusion of D-fenfluramine reduces food intake. Blockade by the 5-HT(1B) antagonist SB-216641. Simansky, K.J., Nicklous, D.M. Pharmacol. Biochem. Behav. (2002) [Pubmed]
A 5-HT7 heteroreceptor-mediated inhibition of [3H]serotonin release in raphe nuclei slices of the rat: evidence for a serotonergic-glutamatergic interaction. Harsing, L.G., Prauda, I., Barkoczy, J., Matyus, P., Juranyi, Z. Neurochem. Res. (2004) [Pubmed]
Role of 5-HT1A and 5-HT1B receptors in the hypophagic effect of 5-HT on the structure of feeding behavior. Mancilla-Diaz, J.M., Escartin-Perez, R.E., Lopez-Alonso, V.E., Floran-Garduño, B., Romano-Camacho, J.B. Med. Sci. Monit. (2005) [Pubmed]

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