Abstract
A novel chemical synthesis of nat- and rac-Prostacyclin (PGI 2 ) and 5,6-dihydro-PGI 2 is described. Like PGI 2 , both stable analogs inhibit human platelet aggregation induced by ADP, Arachidonic Acid (AA), Collagen and Adrenaline. In all forms of aggregation, 5,6 α -dihydro-PGI 2 resulted 10 times more potent than 5,6 β -dihydro-PGI 2 . The potency ratio of 5,6 α -dihydro-PGI 2 to PGI 2 was variably estimated between 1:100, in the case of ADP-induced aggregation, and 1:10 in the case of AA-induced aggregation. The availability of stable mimics of PGI 2 should be of considerable value in future studies of this substance and may have therapeutic implications.
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