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Matches in SemOpenAlex for { <https://semopenalex.org/work/W1976807060> ?p ?o ?g. }

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• W1976807060 abstract "CV-5975, (R)-3-[(S)-1-carboxy-5-(4-piperidyl)pentyl]amino-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-5-acetic acid, was found to inhibit rabbit lung angiotensin converting enzyme (ACE) activity with an IC50 of 3.1 × 10−9 M and a Ki of 2.6 × 10−9 M, inhibit the angiotensin I (A-l)-induced contraction of the guinea pig ileum with an IC50 of 1.3 × 10−8 M, and augment the bradykinin (BK)-induced contraction of the ileum with an AC50 of 9.2 × 10−10 M. The activity of CV-5975 was comparable to or slightly more potent than that of enalaprilat. The overall inhibition constant (Ki*), calculated from a steady-state analysis of enzyme reactions, was 4.4 × 10−12 M for CV-5975; this indicates that the inhibition was about 5 times more potent than that of enalaprilat (2.0 × 10−11 M). In rats, CV-5975 (0.03 and 0.3 mg/kg, i.v. and 3 and 10 mg/kg, p.o.) inhibited the A-l-induced pressor action more potently and for a longer period than did the corresponding doses of enalaprilat and enalapril. CV-5975 and enalapril (3 mg/kg, p.o.) augmented the BK-induced depressor action to a similar extent. In dogs, CV-5975 (0.3 and 1 mg/kg, p.o.) markedly inhibited the A-l-induced pressor action in a dose related manner, and the duration of this inhibitory activity was longer than with the corresponding doses of enalapril. These data provide evidence for the proposal that CV-5975 is a highly potent and long lasting ACE inhibitor." @default.
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• W1976807060 date "1988-01-01" @default.
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• W1976807060 title "Inhibition of Angiotensin Converting Enzyme by (R)-3-[(S)-1-Carboxy-5-(4-Piperidyl)pentyl]amino-4-Oxo-2,3,4,5-Tetrahydro-1,5-Benzothiazepine-5-Acetic Acid (CV-5975), a Non-Sulfhydryl Compound" @default.
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• W1976807060 doi "https://doi.org/10.1254/jjp.48.323" @default.
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