Antiexcitotoxic Agents

Several compounds that interfere with glutamate receptor activation have been developed and tested against experimental animal models of stroke as well as against human clinical trials. The noncompetitive NMDA antagonist MK-801 (dizocilpine) improved outcome in models of focal ischemia, producing up to 75% reductions in infarct volume. Both MK-801 and dextromorphan, another noncompetitive NMDA receptor antagonist, exhibited protective effects in experimental studies, but clinical trials were terminated early because of phencycli-dine-like psychotic side effects and lack of efficacy against stroke injury (Kermer et al., 1999). Some other noncom-petitive (aptiganel, ceresine) or competitive (selfotel, eliprodil) NMDA receptor antagonists were shown to be very effective in animal stroke models, but with no significant effects in clinical trails (Danton and Dietrich, 2004). Non-NMDA antagonists also were being developed and studied against stroke conditions. Zonampanel (YM-872) is an AMPA antagonist and currently is being tested in human phase 2 clinical trails. In addition, another AMPA antagonist SPD-502, as well as metabo-tropic glutamate receptor modulators, are being developed and tested against stroke injury in animals and humans (Danton and Dietrich, 2004; Legos and Barone, 2003). However, the development of anti-excitotoxic agents against stroke has been disappointing.

Blood Pressure Health

Blood Pressure Health

Your heart pumps blood throughout your body using a network of tubing called arteries and capillaries which return the blood back to your heart via your veins. Blood pressure is the force of the blood pushing against the walls of your arteries as your heart beats.Learn more...

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