The effects of beraprost Na, a stable prostacyclin analog, on animal models of stroke.
We evaluated the effects of beraprost Na (Sodium (+-)-(1R*,2R*, 3aS*,8bS*)-2,3,3a,8b-tetrahydro-2-hydroxy-1-[(E)-(3S*)-3- hyd roxy-4-methyl-1- octen-6-ynyl]-1H-cyclopenta[b]benzofuran-5-butylate, beraprost), a stable and orally active prostacyclin (PGI2) analog with potent antiplatelet and vasodilating properties, on two stroke models, namely sudden death induced by arachidonate (AA) in rabbits and spontaneous stroke in stroke-prone spontaneously hypertensive rats (SHRSP). In the AA-induced sudden death model, 30 min after beraprost administration (1 or 3 mg/kg, po), AA was injected into the rabbit internal carotid artery, and incidence of convulsion and sudden death were assessed. Beraprost decreased both incidence of convulsion and mortality of rabbits. In SHRSP, orally administered beraprost (100 micrograms/kg, twice a day from 56-385 d of age) improved survival rate and decreased incidence of stroke. Preventive effects of beraprost on the two stroke models may have been caused mainly by the improvement of cerebral circulation. These results indicate that beraprost may have potential in the treatment and/or prevention of the cerebral circulatory disorders.
Hirano
T
T
Laboratory of Pharmacology, Toray Industries Inc., Kanagawa, Japan.
Yamori
Y
Y
Kanai
N
N
Umetsu
T
T
Nishio
S
S
D000818:Animals; D016718:Arachidonic Acid; D001794:Blood Pressure / Q000187:drug effects; D001835:Body Weight / Q000187:drug effects; D002560:Cerebrovascular Circulation / Q000187:drug effects; D002561:Cerebrovascular Disorders / Q000139:chemically induced / Q000188:drug therapy* / Q000401:mortality; D003645:Death, Sudden; D004110:Diltiazem / Q000627:therapeutic use; D011464:Epoprostenol / Q000031:analogs & derivatives* / Q000494:pharmacology; D008297:Male; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology*; D011817:Rabbits; D051381:Rats; D011918:Rats, Inbred SHR; D013988:Ticlopidine / Q000627:therapeutic use
D010975:Platelet Aggregation Inhibitors; D016718:Arachidonic Acid; C048081:beraprost; D011464:Epoprostenol; D004110:Diltiazem; D013988:Ticlopidine