Ligustrazine (2,3,5,6-tetramethylpyrazine) is a major active ingredient of the Szechwan lovage rhizome and is extensively used in treatment of ischemic
cerebrovascular disease. The mechanism of action of
ligustrazine use against ischemic
cerebrovascular diseases remains unclear at present. This study summarizes its protective effect, the optimum time window of administration, and the most effective mode of administration for clinical treatment of
cerebral ischemia/
reperfusion injury. We examine the effects of
ligustrazine on suppressing
excitatory amino acid release, promoting migration, differentiation and proliferation of endogenous neural stem cells. We also looked at its effects on angiogenesis and how it inhibits
thrombosis, the inflammatory response, and apoptosis after
cerebral ischemia. We consider that
ligustrazine gives noticeable protection from
cerebral ischemia/
reperfusion injury. The time window of
ligustrazine administration is limited. The protective effect and time window of a series of derivative monomers of
ligustrazine such
as 2-[(1,1-dimethylethyl)oxidoimino]methyl]-3,5,6-trimethylpyrazine,
CXC137 and
CXC195 after
cerebral ischemia were better than
ligustrazine.