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2-Methylthioadenosine-5′-phosphate: a Specific Inhibitor of Platelet Aggregation


CERTAIN analogues of adenosine have been found to act both in vivo as vasodilators and in vitro as inhibitors of ADP-mediated platelet aggregation, and Born et al.1 suggested that this dual activity may preclude the potential usefulness of adenosine analogues as antithrombotic agents. Work in this institute with 2-substituted adenosine analogues showed that, although they have both vasodilatory and platelet aggregation inhibitory properties, some analogues, for example, 2-methoxyadenosine and 2-trifluoromethyladenosine, were considerably less potent as inhibitors of platelet aggregation than as vasodilators (Table 1). These observations suggested that it may be possible in suitable analogues to separate the two effects. 2-Methylthioadenosine-5′-phosphate (patent application filed) was found to be a potent inhibitor of ADP-mediated platelet aggregation but to have no discernible effects on the cardiovascular system.

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MICHAL, F., MAGUIRE, M. & GOUGH, G. 2-Methylthioadenosine-5′-phosphate: a Specific Inhibitor of Platelet Aggregation. Nature 222, 1073–1074 (1969).

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