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Neuroprotective Effect of D-(E)-2-amino-4-methyl-5-phosphono-3-pentenoic Acid in the Gerbil Model of Transient Global Cerebral Ischemia

M Okada, H Ueda, M Kometani, K Nakao, Y Kohjimoto, I Takahashi, I Tanaka

Arzneimittelforschung. 1997 Jun;47(6):700-2.

PMID: 9239445

Abstract:

Effect of the new competitive N-methyl-D-aspartate (NMDA) antagonist D-(E)-2-amino-4-methyl-5-phosphono-3-pentenoic acid (CAS 137424-81-8, CGP 40116) was examined in a mongolian gerbil model of global cerebral ischemia. Effect of CGP 40116 was compared to that of another competitive NMDA antagonist, (+/-)-cis-4-phosphonomethyl-piperadine-2-carboxylic acid (CAS 110347-85-8, CGS 19755) under the same conditions. Drugs were administered intraperitoneally 30 min before bilateral carotid artery occlusion. At 4 days after the ischemia, locomotor activity was significantly higher in ischemic control mongolian gerbils in comparison with sham-operated mongolian gerbils. CGP 40116 at the dose of 10 mg/kg and CGS 19755 at the doses of 10 and 30 mg/kg significantly suppressed the increase of the motility. Seven days after ischemia, ischemic control group was still hyperactive compared to sham-operated group. CGP 40116 at the dose of 10 mg/kg and CGS 19755 at the dose of 30 mg/kg significantly reversed it. The number of survived neurons of ischemic control group was significantly less than that of sham-operated group at 7 days after ischemia. CGP 40116 at the dose of 10 mg/kg and CGS 19755 at the dose of 30 mg/kg significantly increased the number of survived neurons. It is concluded that CGP 40116 is more potent for amelioration of global cerebral ischemic damage than CGS 19755.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP79055688-B D-(-)-2-Amino-5-phosphonopentanoic Acid - CAS 79055-68-8 D-(-)-2-Amino-5-phosphonopentanoic Acid - CAS 79055-68-8 79055-68-8 Price
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