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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
 
 
 
 

Inhibition of platelet aggregation by diltiazem. Comparison with verapamil and nifedipine and inhibitory potencies of diltiazem metabolites.

The inhibitory effects of three calcium blockers, diltiazem (d-form), verapamil, and nifedipine, on ADP- and collagen-induced platelet aggregation of human and rabbit platelets were compared. The potency of diltiazem was greater than those of verapamil and nifedipine in human platelet-rich plasma. A similar order of the inhibitory potencies was observed in rabbit platelet-rich plasma, but this order was reversed when washed platelets were aggregated in buffered saline. Antiaggregatory potencies of metabolites on diltiazem and their optical isomers were examined in human platelet-rich plasma. All the metabolites except deacetyl-N-demethyl diltiazem showed greater activity than diltiazem in ADP- or collagen-induced platelet aggregation. The potencies of the l-isomers of the deacetyl-N-demethyl metabolites were greater than those of the d-isomers. On the other hand, the inhibitory effect of the d-isomer of deacetyl-O-demethyl diltiazem was greater than that of the l-form at lower concentrations, whereas the relationship was opposite at higher concentrations. There was no marked difference in antiaggregatory potency between the d- and l-forms of diltiazem and N-demethyl diltiazem.[1]

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