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Chemical Compound Review:

CI-1034 potassium10-(7- ethylbenzo[1,3]dioxol-5...

Synonyms:

Sahi, J. et al., McDuffie, J.E. et al., Coe, Y. et al.

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Disease relevance of 7-(7-ethylbenzo[1,3]dioxol-5-yl)-10,10-dioxo-9-[2-(trifluoromethyl)phenyl]-10$l^{6}-thia-9-azabicyclo[4.4.0]deca-1,3,5,7-tetraene-8-carboxylic acid

CI-1034, an endothelin-A receptor antagonist was being developed for pulmonary hypertension [1].

High impact information on 7-(7-ethylbenzo[1,3]dioxol-5-yl)-10,10-dioxo-9-[2-(trifluoromethyl)phenyl]-10$l^{6}-thia-9-azabicyclo[4.4.0]deca-1,3,5,7-tetraene-8-carboxylic acid

The endothelin A receptor antagonists PD 156707 (CI-1020) and PD 180988 (CI-1034) reverse the hypoxic pulmonary vasoconstriction in the perinatal lamb [2].
In human hepatocytes, no increase in CYP3A4 activity was observed in vitro, while mRNA was induced 15-fold, similar to rifampin, indicating that CI-1034 is both an inhibitor and inducer of CYP3A4 [1].
Immunohistochemistry staining indicated increased expression of inducible nitric oxide synthase (iNOS), cleaved caspase-3, and S100A8/A9 (within in monocytes and neutrophils) proteins in coronary arteries of CI-1034-treated animals [3].
Acute coronary artery injury in dogs following administration of CI-1034, an endothelin A receptor antagonist [3].

Gene context of 7-(7-ethylbenzo[1,3]dioxol-5-yl)-10,10-dioxo-9-[2-(trifluoromethyl)phenyl]-10$l^{6}-thia-9-azabicyclo[4.4.0]deca-1,3,5,7-tetraene-8-carboxylic acid

Metabolism and transporter-mediated drug-drug interactions of the endothelin-A receptor antagonist CI-1034 [1].

References

Metabolism and transporter-mediated drug-drug interactions of the endothelin-A receptor antagonist CI-1034. Sahi, J., Sinz, M.W., Campbell, S., Mireles, R., Zheng, X., Rose, K.A., Raeissi, S., Hashim, M.F., Ye, Y., de Morais, S.M., Black, C., Tugnait, M., Keller, L.H. Chem. Biol. Interact. (2006) [Pubmed]
The endothelin A receptor antagonists PD 156707 (CI-1020) and PD 180988 (CI-1034) reverse the hypoxic pulmonary vasoconstriction in the perinatal lamb. Coe, Y., Haleen, S.J., Welch, K.M., Liu, Y.A., Coceani, F. J. Pharmacol. Exp. Ther. (2002) [Pubmed]
Acute coronary artery injury in dogs following administration of CI-1034, an endothelin A receptor antagonist. McDuffie, J.E., Yu, X., Sobocinski, G., Song, Y., Chupka, J., Albassam, M. Cardiovasc. Toxicol. (2006) [Pubmed]

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