Key result
CGS 35066, a potent and selective endothelin-converting enzyme-1 inhibitor, blocked the big ET-1-induced pressor response in rats by 84% at 90 minutes after a 10 mg/kg intravenous dose.
Absolute Event Rate: 84% vs 50%
CGS 35066 and its prodrug CGS 35339 are novel, potent, and selective ECE-1 inhibitors that may be useful for studying the pathogenic role of ET-1 overproduction.
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May facilitate preclinical ET-1 research in animals; leaves open any clinical translation of ECE-1 inhibition.
Jeng et al. (2000) studied this question. CGS 35066 vs. CGS 26303 was evaluated on Inhibition of the big endothelin-1 (ET-1)-induced pressor response. CGS 35066, a potent and selective endothelin-converting enzyme-1 inhibitor, blocked the big ET-1-induced pressor response in rats by 84% at 90 minutes after a 10 mg/kg intravenous dose.
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