The in vitro effects of a new synthetic tripeptide GYK1 14,451 on platelet aggregation and arachidonic acid metabolism were evaluated. GYKI 14,451 at concentrations as low as 1 μM selectively inhibited platelet aggregation induced by 0.5 U/ml of thrombin. Similarl-malondialdehyde and thromboxane B2 production by platelets stimulated with thrombin were inhibited by the peptide. No inhibitory effect of the peptide was shown when 14C Arachidonic acid metabolism was evaluated in unstimulated platelets. Kinetic studies suggest that GYKI 14,451 interacts with thrombin by an apparently competitive mechanism.

GYKI 14,451, a synthetic tripeptide inhibitor of thrombin: activity on platelet aggregation and arachidonic acid metabolism / E. Tremoli, P. Maderna, S. Colli, E. Agradi, A. Petroni, R. Paoletti. - In: PHARMACOLOGICAL RESEARCH COMMUNICATIONS. - ISSN 0031-6989. - 13:4(1981 Apr), pp. 339-349.

GYKI 14,451, a synthetic tripeptide inhibitor of thrombin: activity on platelet aggregation and arachidonic acid metabolism

E. Tremoli
Primo
;
S. Colli;E. Agradi;A. Petroni
Penultimo
;
R. Paoletti
Ultimo
1981

Abstract

The in vitro effects of a new synthetic tripeptide GYK1 14,451 on platelet aggregation and arachidonic acid metabolism were evaluated. GYKI 14,451 at concentrations as low as 1 μM selectively inhibited platelet aggregation induced by 0.5 U/ml of thrombin. Similarl-malondialdehyde and thromboxane B2 production by platelets stimulated with thrombin were inhibited by the peptide. No inhibitory effect of the peptide was shown when 14C Arachidonic acid metabolism was evaluated in unstimulated platelets. Kinetic studies suggest that GYKI 14,451 interacts with thrombin by an apparently competitive mechanism.
Thrombin; Arachidonic Acids; Platelet Aggregation; Kinetics; Humans; Peptides; Oligopeptides; Thromboxane A2; Malondialdehyde
Settore BIO/14 - Farmacologia
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/188693
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