Structural insights in platelet receptor synergism-antiplatelet therapy in post-ischemic cerebrovascular events

Blood Cells Mol Dis. 2005 May-Jun;34(3):248-56. doi: 10.1016/j.bcmd.2005.01.003.

Abstract

Synergy between agonists of platelet aggregation, namely, ADP and epinephrine, has been studied in patients having a history of cerebrovascular ischemic event. There is a significant variability of responsiveness among individuals towards clopidogrel, which is a specific inhibitor of the low-affinity human purinergic receptor (P2Y12). For responders of clopidogrel, simultaneous application of ADP and epinephrine at sub-threshold concentrations (i.e., concentration below the threshold concentration at which aggregation occurs) leads to platelet aggregation, which is followed by deaggregation. For non-responders of the drug, the synergism seems to be stronger, showing no deaggregatory pattern. The inhibition of synergism by yohimbine hydrochloride (YH), a blocker of alpha2A-adrenoreceptors is more pronounced in non-responders. A simple structural model based on receptor-receptor interaction is proposed to explain the synergism. The model explains synergy in terms of cooperative interaction between the low-affinity ADP receptor P2Y12 (Swiss Prot:Q9H244) and the alpha2A-adrenoreceptor (Swiss Prot:P08913). It follows that the synergistic effect can be achieved in only one of the two 3D structures for the alpha2A-adrenoreceptor P08913 permitted by homology modeling, as there is a better docking interface with the Q9H244. The synergism itself and the observed dichotomous phenomenon in relation to inhibition of synergism among responders and non-responders can be accounted for, if the interacting receptors on the dynamic membrane interface compete with the clopidogrel binding.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine Diphosphate / pharmacology
  • Adrenergic alpha-2 Receptor Antagonists
  • Brain Ischemia / drug therapy
  • Clopidogrel
  • Drug Resistance
  • Drug Synergism
  • Epinephrine / pharmacology
  • Humans
  • Membrane Proteins / antagonists & inhibitors
  • Membrane Proteins / metabolism
  • Models, Molecular
  • Platelet Aggregation / drug effects*
  • Platelet Aggregation Inhibitors / therapeutic use*
  • Purinergic P2 Receptor Antagonists
  • Receptor Cross-Talk*
  • Receptors, Adrenergic, alpha-2 / metabolism
  • Receptors, Purinergic P2 / metabolism
  • Receptors, Purinergic P2Y12
  • Stroke / drug therapy*
  • Ticlopidine / analogs & derivatives*
  • Ticlopidine / therapeutic use

Substances

  • ADRA2A protein, human
  • Adrenergic alpha-2 Receptor Antagonists
  • Membrane Proteins
  • P2RY12 protein, human
  • Platelet Aggregation Inhibitors
  • Purinergic P2 Receptor Antagonists
  • Receptors, Adrenergic, alpha-2
  • Receptors, Purinergic P2
  • Receptors, Purinergic P2Y12
  • Adenosine Diphosphate
  • Clopidogrel
  • Ticlopidine
  • Epinephrine