Ginkgolides are diterpene trilactones with a cage-like skeleton consisting of six five-membered rings and a unique t-Bu group from Ginkgo biloba tree.Many studies have demonstrated that they are highly potent and selective antagonists of platelet activating factor receptor (PAFR) and glycine receptor (GlyR).Ginkgolide skeleton modifications may conduce to physiological activities variation.Therefore, many ginkgolide derivatives and analogs have been synthesized for the optimal antagonistic activities towards PAFR or GlyR.This review covers the structure-activity relationship studies of ginkgolide derivatives and analogs.