New pentamidine related substances which simultaneously inhibit platelet aggregation and accelerate plasmin generation and in vitro clot lysis

Research output: Contribution to journalArticle

Abstract

Pentamidine, a highly toxic drug, possesses RGD-peptide (Arg-Gly-Asp)-like antiplatelet actions. The objective of this investigation was to study the anticipated profibrinolytic and antiplatelet actions of pentamidine and of pentamidine (bearing guanidino-like groups)-related synthetic peptidomimetic compounds. Platelet aggregation inhibition was assessed using ADP, thrombin, collagen, arachidonic acid and epinephrine as inducers, by aggregometry. In vitro chromogenic plasmin generation tests and clot lysis assays were also performed. Two (assigned as D-2 and D-3) of the synthetic pentamidine-guanidino related molecules were able to inhibit platelet aggregation and simultaneously accelerate in vitro plasmin generation and clot-lysis in the nM range. These dual action antithrombotic agents now need to be tested further to assess their antithrombotic actions in vivo.

Original languageEnglish
Pages (from-to)256-258
Number of pages3
JournalBlood Coagulation and Fibrinolysis
Volume7
Issue number2
Publication statusPublished - 1996

Fingerprint

Pentamidine
Fibrinolysin
Platelet Aggregation
Peptidomimetics
Fibrinolytic Agents
Poisons
Arachidonic Acid
Thrombin
Adenosine Diphosphate
Epinephrine
Collagen
In Vitro Techniques
Pharmaceutical Preparations

Keywords

  • Antiplatelet effect
  • Guanidino group
  • Pentamidine
  • Profibrinolytic effect
  • RGD

ASJC Scopus subject areas

  • Hematology

Cite this

@article{29f3230af46743c9a17faec481b07a7c,
title = "New pentamidine related substances which simultaneously inhibit platelet aggregation and accelerate plasmin generation and in vitro clot lysis",
abstract = "Pentamidine, a highly toxic drug, possesses RGD-peptide (Arg-Gly-Asp)-like antiplatelet actions. The objective of this investigation was to study the anticipated profibrinolytic and antiplatelet actions of pentamidine and of pentamidine (bearing guanidino-like groups)-related synthetic peptidomimetic compounds. Platelet aggregation inhibition was assessed using ADP, thrombin, collagen, arachidonic acid and epinephrine as inducers, by aggregometry. In vitro chromogenic plasmin generation tests and clot lysis assays were also performed. Two (assigned as D-2 and D-3) of the synthetic pentamidine-guanidino related molecules were able to inhibit platelet aggregation and simultaneously accelerate in vitro plasmin generation and clot-lysis in the nM range. These dual action antithrombotic agents now need to be tested further to assess their antithrombotic actions in vivo.",
keywords = "Antiplatelet effect, Guanidino group, Pentamidine, Profibrinolytic effect, RGD",
author = "M. Udvardy and E. Posan and J. H{\'a}rsfalvi and Z. Dinya",
year = "1996",
language = "English",
volume = "7",
pages = "256--258",
journal = "Blood Coagulation and Fibrinolysis",
issn = "0957-5235",
publisher = "Lippincott Williams and Wilkins",
number = "2",

}

TY - JOUR

T1 - New pentamidine related substances which simultaneously inhibit platelet aggregation and accelerate plasmin generation and in vitro clot lysis

AU - Udvardy, M.

AU - Posan, E.

AU - Hársfalvi, J.

AU - Dinya, Z.

PY - 1996

Y1 - 1996

N2 - Pentamidine, a highly toxic drug, possesses RGD-peptide (Arg-Gly-Asp)-like antiplatelet actions. The objective of this investigation was to study the anticipated profibrinolytic and antiplatelet actions of pentamidine and of pentamidine (bearing guanidino-like groups)-related synthetic peptidomimetic compounds. Platelet aggregation inhibition was assessed using ADP, thrombin, collagen, arachidonic acid and epinephrine as inducers, by aggregometry. In vitro chromogenic plasmin generation tests and clot lysis assays were also performed. Two (assigned as D-2 and D-3) of the synthetic pentamidine-guanidino related molecules were able to inhibit platelet aggregation and simultaneously accelerate in vitro plasmin generation and clot-lysis in the nM range. These dual action antithrombotic agents now need to be tested further to assess their antithrombotic actions in vivo.

AB - Pentamidine, a highly toxic drug, possesses RGD-peptide (Arg-Gly-Asp)-like antiplatelet actions. The objective of this investigation was to study the anticipated profibrinolytic and antiplatelet actions of pentamidine and of pentamidine (bearing guanidino-like groups)-related synthetic peptidomimetic compounds. Platelet aggregation inhibition was assessed using ADP, thrombin, collagen, arachidonic acid and epinephrine as inducers, by aggregometry. In vitro chromogenic plasmin generation tests and clot lysis assays were also performed. Two (assigned as D-2 and D-3) of the synthetic pentamidine-guanidino related molecules were able to inhibit platelet aggregation and simultaneously accelerate in vitro plasmin generation and clot-lysis in the nM range. These dual action antithrombotic agents now need to be tested further to assess their antithrombotic actions in vivo.

KW - Antiplatelet effect

KW - Guanidino group

KW - Pentamidine

KW - Profibrinolytic effect

KW - RGD

UR - http://www.scopus.com/inward/record.url?scp=0029893126&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0029893126&partnerID=8YFLogxK

M3 - Article

VL - 7

SP - 256

EP - 258

JO - Blood Coagulation and Fibrinolysis

JF - Blood Coagulation and Fibrinolysis

SN - 0957-5235

IS - 2

ER -