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Evaluation of annexin V as a platelet-directed thrombus targeting agent.

Abstract
Annexin V is a human phospholipid binding protein (M(r) 36,000) that binds with high affinity to activated platelets in vitro. We studied the biodistribution and thrombus binding of annexin V in rabbit and swine models of fully occlusive arterial thrombi formed 1-2 h prior to injection of annexin V. Iodinated annexin V was cleared from blood in a rapid early phase (t1/2 = 6.4 min, 76% of radioactivity) and a slower late phase (t1/2 = 71 min, 24% of radioactivity). Organ uptake was highest in the kidney and spleen and lowest in heart and skeletal muscle. Thrombus/blood uptake ratios were (mean +/- SEM): 6.39 +/- 1.80 for rabbit iliac artery, 6.97 +/- 1.45 for swine carotid artery, and 7.68 +/- 1.70 for swine femoral artery (all p values < 0.01 versus control artery); a control protein, ovalbumin, showed an uptake ratio of 0.59 +/- 0.08 in swine femoral artery thrombi. These results indicate that annexin V is useful as an agent for selective targeting of platelet-containing thrombi.
AuthorsJ F Tait, M D Cerqueira, T A Dewhurst, K Fujikawa, J L Ritchie, J R Stratton
JournalThrombosis research (Thromb Res) Vol. 75 Issue 5 Pg. 491-501 (Sep 01 1994) ISSN: 0049-3848 [Print] United States
PMID7992250 (Publication Type: Journal Article, Research Support, U.S. Gov't, P.H.S.)
Chemical References
  • Annexin A5
  • Iodine Radioisotopes
Topics
  • Animals
  • Annexin A5 (blood, pharmacokinetics, pharmacology)
  • Biological Availability
  • Biological Transport (physiology)
  • Blood Platelets (drug effects, metabolism, physiology)
  • Carotid Arteries (metabolism, pathology, physiology)
  • Carotid Artery Thrombosis (metabolism, pathology, physiopathology)
  • Disease Models, Animal
  • Female
  • Iliac Artery (embryology, pathology, physiology)
  • Iodine Radioisotopes
  • Kidney (embryology, pathology, physiology)
  • Male
  • Muscle, Skeletal (metabolism, pathology, physiology)
  • Rabbits
  • Spleen (metabolism, pathology, physiology)
  • Swine
  • Thrombosis (blood, metabolism, physiopathology)

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