A novel chemical synthesis of nat- and rac-Prostacyclin (PGI2) and 5,6-dihydro-PGI2 is described. Like PGI2, both stable analogs inhibit human platelet aggregation induced by ADP, Arachidonic Acid (AA), Collagen and Adrenaline. In all forms of aggregation, 5,6α-dihydro-PGI2 resulted 10 times more potent than 5,6β-dihydro-PGI2. The potency ratio of 5,6α-dihydro-PGI2 to PGI2 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 PGI2 should be of considerable value in future studies of this substance and may have therapeutic implications. © 1977 The Italian Pharmacological Society.
Inhibition of human platelet aggregation by stable analogs of prostacyclin / Togna, Giuseppina Ines; C., Gandolfi; A., Andreoni; A., Fumagalli; C., Passarotti; F., Faustini; Patrono, Carlo. - In: PHARMACOLOGICAL RESEARCH COMMUNICATIONS. - ISSN 0031-6989. - STAMPA. - 9:10(1977), pp. 909-916.
Inhibition of human platelet aggregation by stable analogs of prostacyclin
TOGNA, Giuseppina Ines;PATRONO, CARLO
1977
Abstract
A novel chemical synthesis of nat- and rac-Prostacyclin (PGI2) and 5,6-dihydro-PGI2 is described. Like PGI2, both stable analogs inhibit human platelet aggregation induced by ADP, Arachidonic Acid (AA), Collagen and Adrenaline. In all forms of aggregation, 5,6α-dihydro-PGI2 resulted 10 times more potent than 5,6β-dihydro-PGI2. The potency ratio of 5,6α-dihydro-PGI2 to PGI2 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 PGI2 should be of considerable value in future studies of this substance and may have therapeutic implications. © 1977 The Italian Pharmacological Society.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.