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

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.

Authors+Show Affiliations

Drug Discovery Research Unit, Ciba-Geigy Japan Ltd., Takarazuka, Japan.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

9239445

Citation

Okada, M, et al. "Neuroprotective Effect of D-(E)-2-amino-4-methyl-5-phosphono-3-pentenoic Acid in the Gerbil Model of Transient Global Cerebral Ischemia." Arzneimittel-Forschung, vol. 47, no. 6, 1997, pp. 700-2.
Okada M, Ueda H, Kometani M, et al. Neuroprotective effect of D-(E)-2-amino-4-methyl-5-phosphono-3-pentenoic acid in the gerbil model of transient global cerebral ischemia. Arzneimittelforschung. 1997;47(6):700-2.
Okada, M., Ueda, H., Kometani, M., Nakao, K., Kohjimoto, Y., Takahashi, I., & Tanaka, I. (1997). Neuroprotective effect of D-(E)-2-amino-4-methyl-5-phosphono-3-pentenoic acid in the gerbil model of transient global cerebral ischemia. Arzneimittel-Forschung, 47(6), 700-2.
Okada M, et al. Neuroprotective Effect of D-(E)-2-amino-4-methyl-5-phosphono-3-pentenoic Acid in the Gerbil Model of Transient Global Cerebral Ischemia. Arzneimittelforschung. 1997;47(6):700-2. PubMed PMID: 9239445.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Neuroprotective effect of D-(E)-2-amino-4-methyl-5-phosphono-3-pentenoic acid in the gerbil model of transient global cerebral ischemia. AU - Okada,M, AU - Ueda,H, AU - Kometani,M, AU - Nakao,K, AU - Kohjimoto,Y, AU - Takahashi,I, AU - Tanaka,I, PY - 1997/6/1/pubmed PY - 1997/6/1/medline PY - 1997/6/1/entrez SP - 700 EP - 2 JF - Arzneimittel-Forschung JO - Arzneimittelforschung VL - 47 IS - 6 N2 - 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. SN - 0004-4172 UR - https://www.unboundmedicine.com/medline/citation/9239445/Neuroprotective_effect_of_D__E__2_amino_4_methyl_5_phosphono_3_pentenoic_acid_in_the_gerbil_model_of_transient_global_cerebral_ischemia_ L2 - https://medlineplus.gov/transientischemicattack.html DB - PRIME DP - Unbound Medicine ER -