Calcium antagonist PY 108-068: demonstration of its efficacy in various types of experimental brain ischemia.
The protective properties of PY 108-068 against ischemic disturbances in the brain were investigated in vitro and in vivo. The calcium antagonistic effects were demonstrated on isolated, calcium-loaded arterial rings of feline cerebral arteries. Determination of brain tissue oxygenation with pO2 microelectrodes showed that PY 108-068 improved oxygen supply in the cortex of cats subjected to epicerebral arterial occlusion. In a model of cerebral vasospasm induced by autologous blood superfusion, PY 108-068 reversed the spastic state of cortical microvessels. In a chronic stroke model (microsphere embolization in rats) PY 108-068 led to a significant reduction in mortality and in the severity of neurological symptoms, whereby the peroral efficacy of the drug could be demonstrated. The efficacy of PY 108-068 in a variety of ischemic insults makes this drug a promising aid in the treatment of cerebrovascular accidents.
D000818:Animals; D001834:Body Water / Q000032:analysis; D002545:Brain Ischemia / Q000188:drug therapy*; D002121:Calcium Channel Blockers / Q000627:therapeutic use*; D002415:Cats; D002540:Cerebral Cortex / Q000032:analysis; D066298:In Vitro Techniques; D002542:Intracranial Embolism and Thrombosis / Q000188:drug therapy; D002546:Ischemic Attack, Transient / Q000188:drug therapy; D009543:Nifedipine / Q000031:analogs & derivatives* / Q000627:therapeutic use; D010100:Oxygen / Q000032:analysis; D010313:Partial Pressure; D051381:Rats; D011916:Rats, Inbred F344
D002121:Calcium Channel Blockers; D009543:Nifedipine; C034600:darodipine; D010100:Oxygen