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Chemical Compound Review:

CHEMBL87778 2,5-dibutyl-4-[[4-[2-(2H- tetrazol-5...

Synonyms: AG-D-68755, SureCN7398914, ACMC-20mv1m, CHEBI:238592, AC1L2ZJY, ...

Olins, G.M. et al., Schuh, J.R. et al., Morrissey, J.J. et al., Olins, G.M. et al.

Morrissey, Klahr,

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Disease relevance of SC-51316

To investigate the mechanism by which angiotensin-converting enzyme (ACE) inhibition attenuates atherogenesis, we have studied the effects of a non-sulfhydryl ACE inhibitor, enalapril, and an angiotensin receptor antagonist, SC-51316, in cholesterol-fed rabbits [1].

High impact information on SC-51316

In vitro pharmacology of a nonpeptidic angiotensin II receptor antagonist, SC-51316 [2].
In addition, SC-51316 inhibited AII-induced aldosterone release from rat adrenal zona glomerulosa cells and blocked inhibition of renin release by AII from rat kidney slices with pA2 values of 8.62 and 8.9, respectively [2].
SC-51316 inhibited [125I]AII binding selectively to the AT1 receptor with IC50 values of 3.6 and 5.1 nM in rat adrenal cortical and rat uterine membrane preparations, respectively [2].
In conscious, sodium-deficient dogs, administration of SC-51316 (30 mg/kg orally) or enalapril (10 mg/kg orally) lowered blood pressure similarly over a 24 h observation period [3].
SC-51316 had no effect on heart rate [3].

Gene context of SC-51316

Enalapril or SC-51316 treatment had no significant effect on ICAM-1 mRNA levels [4].
Enalapril significantly blunted the increase in VCAM-1 mRNA levels and VCAM-1 protein determined by immunocytochemistry; SC-51316 had no significant effect [4].

References

Differential effects of renin-angiotensin system blockade on atherogenesis in cholesterol-fed rabbits. Schuh, J.R., Blehm, D.J., Frierdich, G.E., McMahon, E.G., Blaine, E.H. J. Clin. Invest. (1993) [Pubmed]
In vitro pharmacology of a nonpeptidic angiotensin II receptor antagonist, SC-51316. Olins, G.M., Corpus, V.M., McMahon, E.G., Palomo, M.A., Schuh, J.R., Blehm, D.J., Huang, H.C., Reitz, D.B., Manning, R.E., Blaine, E.H. J. Pharmacol. Exp. Ther. (1992) [Pubmed]
In vivo pharmacology of SC-51316, a nonpeptidic angiotensin II receptor antagonist. Olins, G.M., Smits, G.J., Koepke, J.P., Huang, H.C., Reitz, D.B., Manning, R.E., Blaine, E.H. Am. J. Hypertens. (1993) [Pubmed]
Differential effects of ACE and AT1 receptor inhibition on chemoattractant and adhesion molecule synthesis. Morrissey, J.J., Klahr, S. Am. J. Physiol. (1998) [Pubmed]

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