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Reversible or irreversible modification of [3H]PAF binding on rabbit platelet membranes differentiates various PAF receptor antagonists.
Lipids. 1992 Aug; 27(8):582-6.L

Abstract

[3H]Platelet-activating factor (PAF) binding to rabbit platelet membranes was examined before and after 20 min preincubation at 25 degrees C in the presence of PAF, lysoPAF, or of five different PAF receptor antagonists (L 652731, BN 52021, WEB 2086, BN 52111 and BN 52115). When platelet membranes were not washed after preincubation with PAF or PAF antagonists, no significant specific binding of [3H]PAF was observed, which suggests full occupancy of the binding sites. When membranes were extensively washed, full recovery of specific [3H]PAF binding was attained with L 652731 and partial recoveries (60%, 55% and 30%) were reached with BN 52021, WEB 2086 and PAF, respectively; no recovery was seen with the dioxolanes BN 52111 and BN 52115. Scatchard analysis of the binding data indicated that no significant change in the dissociation constant (Kd) and maximum number of binding sites (Bmax) occurred after preincubation of platelet membrane with L 652731, whereas a reduction of Bmax was observed when PAF and BN 52021 were measured. When platelet membranes were preincubated with WEB 2086, Bmax and Kd significantly increased. The data suggest differing binding properties for PAF and the PAF antagonists. Some of the PAF antagonists may tightly bind to the PAF receptor site(s) and/or irreversibly modify or downregulate PAF recognition sites. Our results also suggest that the interaction of PAF receptor antagonists with PAF receptor can be divided into at least two components, namely a reversible component and an irreversible one.

Authors+Show Affiliations

Institut Henri Beaufour, Les Ulis, France.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

1328798

Citation

Domingo, M T., et al. "Reversible or Irreversible Modification of [3H]PAF Binding On Rabbit Platelet Membranes Differentiates Various PAF Receptor Antagonists." Lipids, vol. 27, no. 8, 1992, pp. 582-6.
Domingo MT, Piro F, Broquet C, et al. Reversible or irreversible modification of [3H]PAF binding on rabbit platelet membranes differentiates various PAF receptor antagonists. Lipids. 1992;27(8):582-6.
Domingo, M. T., Piro, F., Broquet, C., Auclair, E., Chabrier, P. E., & Braquet, P. (1992). Reversible or irreversible modification of [3H]PAF binding on rabbit platelet membranes differentiates various PAF receptor antagonists. Lipids, 27(8), 582-6.
Domingo MT, et al. Reversible or Irreversible Modification of [3H]PAF Binding On Rabbit Platelet Membranes Differentiates Various PAF Receptor Antagonists. Lipids. 1992;27(8):582-6. PubMed PMID: 1328798.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Reversible or irreversible modification of [3H]PAF binding on rabbit platelet membranes differentiates various PAF receptor antagonists. AU - Domingo,M T, AU - Piro,F, AU - Broquet,C, AU - Auclair,E, AU - Chabrier,P E, AU - Braquet,P, PY - 1992/8/1/pubmed PY - 1992/8/1/medline PY - 1992/8/1/entrez SP - 582 EP - 6 JF - Lipids JO - Lipids VL - 27 IS - 8 N2 - [3H]Platelet-activating factor (PAF) binding to rabbit platelet membranes was examined before and after 20 min preincubation at 25 degrees C in the presence of PAF, lysoPAF, or of five different PAF receptor antagonists (L 652731, BN 52021, WEB 2086, BN 52111 and BN 52115). When platelet membranes were not washed after preincubation with PAF or PAF antagonists, no significant specific binding of [3H]PAF was observed, which suggests full occupancy of the binding sites. When membranes were extensively washed, full recovery of specific [3H]PAF binding was attained with L 652731 and partial recoveries (60%, 55% and 30%) were reached with BN 52021, WEB 2086 and PAF, respectively; no recovery was seen with the dioxolanes BN 52111 and BN 52115. Scatchard analysis of the binding data indicated that no significant change in the dissociation constant (Kd) and maximum number of binding sites (Bmax) occurred after preincubation of platelet membrane with L 652731, whereas a reduction of Bmax was observed when PAF and BN 52021 were measured. When platelet membranes were preincubated with WEB 2086, Bmax and Kd significantly increased. The data suggest differing binding properties for PAF and the PAF antagonists. Some of the PAF antagonists may tightly bind to the PAF receptor site(s) and/or irreversibly modify or downregulate PAF recognition sites. Our results also suggest that the interaction of PAF receptor antagonists with PAF receptor can be divided into at least two components, namely a reversible component and an irreversible one. SN - 0024-4201 UR - https://www.unboundmedicine.com/medline/citation/1328798/Reversible_or_irreversible_modification_of_[3H]PAF_binding_on_rabbit_platelet_membranes_differentiates_various_PAF_receptor_antagonists_ L2 - https://onlinelibrary.wiley.com/resolve/openurl?genre=article&sid=nlm:pubmed&issn=0024-4201&date=1992&volume=27&issue=8&spage=582 DB - PRIME DP - Unbound Medicine ER -