Mechanism involved in the antiplatelet activity of naloxone in human platelets

Joen Rong Sheu, Wei Chun Hung, Ling Wen Lee, Pei Te Chang, Ya Chen Kan, Mao Hsiung Yen

Research output: Contribution to journalArticle

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Abstract

In this study, naloxone was tested for its antiplatelet activity in human platelet suspensions. In platelet suspensions (4.5 x 108/ml), naloxone (0.1-0.5 mM) significantly inhibited platelet aggregation and ATP-release stimulated by various agonists (i.e., thrombin, collagen, U46619, and ADP). Furthermore, naloxone (0.5 and 0.8 mM) dose-dependently inhibited the intracellular free Ca2+ rise of Fura 2-AM loaded platelets stimulated by collagen. Additionally, naloxone (0.5 and 1.0 mM) did not influence the binding of FITC-triflavin to platelet glycoprotein (GP) IIb/IIIa complex. On the other hand, naloxone (0.5 mM) markedly decreased the fluorescence of platelet membranes tagged with diphenylhexatriene (DPH). In addition, naloxone (0.1-0.5 mM) did not significantly affect cyclic-AMP levels in human washed platelets. It is concluded that the antiplatelet activity of naloxone may possibly be due to the induction of conformational changes in the platelet membrane and the inhibition of the intracellular Ca2+ ([Ca2+]i) mobilization as well as the release reaction of platelets stimulated by agonists.

Original languageEnglish
Pages (from-to)12-16
Number of pages5
JournalBiochemical and Biophysical Research Communications
Volume231
Issue number1
DOIs
Publication statusPublished - Feb 3 1997
Externally publishedYes

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Naloxone
Platelets
Blood Platelets
Suspensions
Collagen
Diphenylhexatriene
Integrin beta3
15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid
Intracellular Membranes
Platelet Glycoprotein GPIIb-IIIa Complex
Platelet Membrane Glycoproteins
Membranes
Fluorescein-5-isothiocyanate
Fura-2
Platelet Aggregation
Human Activities
Thrombin
Cyclic AMP
Adenosine Diphosphate
Adenosine Triphosphate

ASJC Scopus subject areas

  • Biochemistry
  • Biophysics
  • Molecular Biology

Cite this

Mechanism involved in the antiplatelet activity of naloxone in human platelets. / Sheu, Joen Rong; Hung, Wei Chun; Lee, Ling Wen; Chang, Pei Te; Kan, Ya Chen; Yen, Mao Hsiung.

In: Biochemical and Biophysical Research Communications, Vol. 231, No. 1, 03.02.1997, p. 12-16.

Research output: Contribution to journalArticle

Sheu, Joen Rong ; Hung, Wei Chun ; Lee, Ling Wen ; Chang, Pei Te ; Kan, Ya Chen ; Yen, Mao Hsiung. / Mechanism involved in the antiplatelet activity of naloxone in human platelets. In: Biochemical and Biophysical Research Communications. 1997 ; Vol. 231, No. 1. pp. 12-16.
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