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Mechanisms of Stimulus—Response Coupling in Platelets pp 83–96Cite as

Specific Binding of [3H]-1-O-Octadecyl Paf-Acether to Washed Human Platelets

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Part of the book series: Advances in Experimental Medicine and Biology ((AEMB,volume 192))

Abstract

[3H]-Paf-acether binds to washed human platelets in a dose-dependent manner. Scatchard analysis reveals two distinct binding sites; a high affinity site with a KD value of 0.259±0.033nM (245+30 sites per platelet) and a lower affinity site with a KD value of 9.22±1.17 nM (1616±165 sites per platelet). Association of 3H-Paf-acether to the high affinity receptor is rapid, being maximal within two minutes and remaining constant for at least twenty minutes. Dissociation from the low affinity receptor is also rapid (t½:<10s) whereas dissociation from the high affinity site is significantly slower (t½: ≈ 70s). [3H]-Paf-acether binding is inhibited by unlabelled (R)-C16-Paf (IC50: 0.08±0.01 nM) > (R)-C18-Paf (0.48±0.03 nM)>(RS)-C18-Paf (1.06±0.19 nM), but remains unchanged in the presence of lyso-C18-Paf at 3.0–300 nM. [3H]-Paf-acether binding and its inhibition by unlabelled (R)-C18-Paf-acether is independent of buffer Ca2+ within the range 0–5.0mM.

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Author information

Authors and Affiliations

  1. Dept. of Biology, Searle Research and Development, High Wycombe, Bucks., UK

    D. P. Tuffin, P. Davey, R. L. Dyer, D. O. Lunt & P. J. Wade

Authors
  1. D. P. Tuffin
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  2. P. Davey
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  3. R. L. Dyer
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  4. D. O. Lunt
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  5. P. J. Wade
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Editor information

Editors and Affiliations

  1. Department of Pharmacology, Royal College of Surgeons, London, England

    J. Westwick

  2. Thrombosis Research Unit, King’s College School of Medicine and Dentistry, London, England

    M. F. Scully  & V. V. Kakkar  & 

  3. Department of Pharmacology, University of Glasgow, Glasgow, Scotland

    D. E. MacIntyre

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© 1985 Plenum Press, New York

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Tuffin, D.P., Davey, P., Dyer, R.L., Lunt, D.O., Wade, P.J. (1985). Specific Binding of [3H]-1-O-Octadecyl Paf-Acether to Washed Human Platelets. In: Westwick, J., Scully, M.F., MacIntyre, D.E., Kakkar, V.V. (eds) Mechanisms of Stimulus—Response Coupling in Platelets. Advances in Experimental Medicine and Biology, vol 192. Springer, Boston, MA. https://doi.org/10.1007/978-1-4615-9442-0_7

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  • DOI: https://doi.org/10.1007/978-1-4615-9442-0_7

  • Publisher Name: Springer, Boston, MA

  • Print ISBN: 978-1-4615-9444-4

  • Online ISBN: 978-1-4615-9442-0

  • eBook Packages: Springer Book Archive

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