Activation of platelets plays a central role in hemostasis as well as in va
rious thromboembolic diseases like myocardial infarction or stroke. Most pl
atelet activating stimuli function through receptors which couple to hetero
trimeric G proteins of the G(i), G(q) and G(12) families. Recent studies ha
ve elucidated the roles of individual G proteins in the regulation of plate
let functions like shape change, aggregation and granule secretion. The sig
naling pathways mediated by heterotrimeric G proteins operate synergistical
ly to induce a full activation of platelets. This review summarizes recent
progress in the understanding of upstream regulation of platelet activation
through G protein-coupled receptors.