The world's first wiki where authorship really matters (Nature Genetics, 2008). Due credit and reputation for authors. Imagine a global collaborative knowledge base for original thoughts. Search thousands of articles and collaborate with scientists around the globe.

wikigene or wiki gene protein drug chemical gene disease author authorship tracking collaborative publishing evolutionary knowledge reputation system wiki2.0 global collaboration genes proteins drugs chemicals diseases compound
Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
Chemical Compound Review

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

Synonyms: AC1MMVTS, CHEMBL20963, SureCN2360553, S8942_SIGMA, BPBio1_000134, ...
 
 
Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.
 

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

 

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

  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. 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]
  2. 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]
  3. 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]
  4. 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]
  5. 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]
 
WikiGenes - Universities