Key result
C2-substituted ADP analogues bind less strongly to high-affinity platelet sites than unsubstituted analogues.
In vitro binding affinities of ADP analogues to fixed platelets correlate with their reported potencies as agonists or antagonists.
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In vitro platelet binding predicts ADP analogue potency; hypothesis-generating for P2Y-targeted agents with no clinical implications yet.
Agarwal et al. (1989) studied this question. ADP analogues was evaluated on Binding affinity (Ki) to high and low affinity sites. C2-substituted ADP analogues bound less strongly (Ki > 2 microM) than analogues without purine ring substituents (Ki < 0.7 microM) at high affinity binding sites on fixed platelets.
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