Design and synthesis of new antagonist peptides for platelet GPIIb/IIIa receptor as anti-thrombotic agents

Bioorganic and Medicinal Chemistry Letters

Volumn 6, Issue 12, 1996, Pages 1351-1356

  Hayashi, Yoshio ^a   Sato, Yoshimi ^a   Katada, Jun ^a   Takiguchi, Yoshimi ^a   Ojima, Iwao ^b   Uno, Isao ^a  

^a NIPPON STEEL CORPORATION   (Japan)

^b STONY BROOK UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTICOAGULANT AGENT; FIBRINOGEN RECEPTOR ANTAGONIST; HEPARIN; LIGAND; OROTYLSERYLARGINYLGLYCYLASPARTYLTRYPTOPHAN; UNCLASSIFIED DRUG;

AMINO TERMINAL SEQUENCE; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CONTROLLED STUDY; DOSE RESPONSE; DRUG DESIGN; DRUG SYNTHESIS; EXTRACORPOREAL CIRCULATION; HUMAN; INTRAVENOUS DRUG ADMINISTRATION; MOUSE; NONHUMAN; POSTOPERATIVE HEMORRHAGE; STRUCTURE ACTIVITY RELATION; THROMBOCYTE AGGREGATION; THROMBOCYTE DYSFUNCTION; THROMBOSIS;

EID: 0029941208     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/0960-894X(96)00224-7     Document Type: Article

References (23)

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21. 18 analytical column; 4.6 mm × 150 mm). To examine the stability of the peptides in vivo, each peptide was administered intravenously (1mg/kg) via a tail vein of ICR mice. Plasma concentrations of the peptides at various time points were determined by HPLC analysis as mentioned above.
22. Male hartley guinea pigs weighing 230-330 g were anesthetized with pentobarbital (35 mg/kg, i.p.). Polyethylene tubes filled with saline containing 100 units/ml heparin were then inserted into the left jugular vein and the right carotid artery and these two tubes were connected with a silicon tube filled with the same solution. The whole length of this shunt was 6 cm. Anti-thrombotic agents were infused via a cannula at the right jugular vein at the rate of 2 ml/hr for 70 min. Ten min after the onset of the infusion, a silk thread was inserted into the shunt. Every 20 min a silk thread was replaced and its wet weight was measured. After the termination of the infusion, the measurement of the thread weight every 20 min was continued for another 60 min. The thrombus weight was calculated from the wet weight of the thread before and after the experiment, and the total thrombus weight was the sum of three thrombus weights obtained during the infusion period or post-infusion period.
23. Katada, J.; Takiguchi, Y.; Muramatsu, M.; Fujiyoshi, T.; Uno, I. Thromb. Res. manuscript submitted.