Research progress of the therapeutic effects of fasudil,a Rho kinase inhibitor and its analogs,on central nervous system diseases

Fasudil,which is initially defined as a novel calcium antagonist,has been clinically applied since 1995 for the treatment of cerebral vasospasm after hemorrhage in the subarachnoid space in Japan.The mechanism of action has not been clarified until Rho kinase(ROCK) was found.This drug exerts strong vasodilative effect through inhibiting ROCK.Recently,increasing evidence indicates that fasudil as a neuroprotective agent can markedly exert therapeutic effect on central nervous system disorders,such as spinal cord injury,Alzheimer disease and multiple sclerosis,and so on.To improve the selectivity of fasudil to ROCK,a number of analogs have been synthesized based on its structure,and proved to be more potent or more selective than fasudil.Herein,the potential of fasudil in the treatment for central nervous system disorders and the study of its analogs were summarized.Moreover,the combination strategies of fasudil were also discussed.