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Chemical Compound Review

Tocris-1838     (2S)-2-[[(2R)-2-[(3,5- dimethylphenyl)carbo...

Synonyms: CHEMBL72410, IRL-2500, SureCN7444422, IRL2500, CHEBI:214250, ...
 
 
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High impact information on Tocris-1838

  • IRL2500 (KD ETA = 30.0 +/- 20.8 microM and KD ETA = 55.6 +/- 9.93 microM) in human and rat left ventricle, respectively [1].
  • The affinity of ETB receptors for sarafotoxin S6c, BQ788 and IRL2500 differed in human and rat left ventricle [1].
  • Sarafotoxin S6c, ET-3, BQ788 and IRL2500 competed against [125I]-PD151242 (ETA selective radioligand) with low affinity in human left ventricle, confirming the ETB selectivity of these compounds [1].
  • In the presence of IRL2500, a selective ET(B)-receptor antagonist, ET-1 was more potent in endothelium-denuded arteries of CHF rats, while this difference was not seen in sham arteries [2].

References

  1. Characterization of the binding of endothelin ETB selective ligands in human and rat heart. Russell, F.D., Davenport, A.P. Br. J. Pharmacol. (1996) [Pubmed]
  2. Enhanced endothelin-1-induced contractions in mesenteric arteries from rats with congestive heart failure: role of ET(B) receptors. Bergdahl, A., Valdemarsson, S., Adner, M., Sun, X.Y., Hedner, T., Edvinsson, L. Eur. J. Heart Fail. (2001) [Pubmed]
 
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