The effect of a peptide aldehyde reversible inhibitor of elastase on a human leucocyte elastase-induced model of emphysema in the hamster

The peptide aldehyde Ro 31-3537, N alpha-(1-adamantanesulphonyl)-N epsilon-(4-carboxybenzoyl)-L-lysyl-L-alanyl-L- valinal, is a reversible competitive, hydrophilic, specific inhibitor of elastase. Its Ki against human leucocyte elastase is 6 x 10(-8) M. The effect of this compound has been studied o...

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Bibliographic Details
Published inEuropean journal of respiratory diseases Vol. 71; no. 5; p. 472
Main Authors Kennedy, A J, Cline, A, Ney, U M, Johnson, W H, Roberts, N A
Format Journal Article
LanguageEnglish
Published Denmark 01.11.1987
Subjects
Adamantane - analogs & derivatives
Adamantane - pharmacology
Animals
Cricetinae
Disease Models, Animal
Leukocyte Elastase
Lung - pathology
Lung Compliance - drug effects
Male
Mesocricetus
Oligopeptides - pharmacology
Pancreatic Elastase - antagonists & inhibitors
Pancreatic Elastase - metabolism
Pulmonary Emphysema - chemically induced
Pulmonary Emphysema - drug therapy
Pulmonary Emphysema - pathology
Respiratory Function Tests
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Summary:The peptide aldehyde Ro 31-3537, N alpha-(1-adamantanesulphonyl)-N epsilon-(4-carboxybenzoyl)-L-lysyl-L-alanyl-L- valinal, is a reversible competitive, hydrophilic, specific inhibitor of elastase. Its Ki against human leucocyte elastase is 6 x 10(-8) M. The effect of this compound has been studied on a model of emphysema in the hamster induced by multiple sequential intratracheal doses of human leucocyte elastase. Concomitant intratracheal dosing of 200 micrograms of inhibitor with the enzyme significantly reduces lung damage as measured by quasi-static lung compliance and by histological assessment of the emphysema.
ISSN:0106-4339