Glutamate carboxypeptidase II (GCPII) inhibitor displays anti-glutamate and anti-cocaine effects in an invertebrate assay

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• 作者：Chris Tallarida (1)
  Kevin Song (1)
  Robert B. Raffa (1)
  Scott M. Rawls (12) scott.rawls@temple.edu
• 关键词：GCPII – ; Glutamate – ; 2 ; PMPA – ; Cocaine – ; Planaria – ; NMDA – ; Pilocarpine – ; Stereotypy
• 刊名：Amino Acids
• 出版年：2012
• 出版时间：June 2012
• 年：2012
• 卷：42
• 期：6
• 页码：2521-2524
• 全文大小：244.9 KB
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  11. Rawls SM, Karaca F, Madhani I, Bhojani V, Martinez RL, Abou-Gharbia M, Raffa RB (2010) β-lactamase inhibitors display anti-seizure properties in an invertebrate assay. Neuroscience 169:1800–1804
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  14. Slusher BS, Thomas A, Paul M, Schad CA, Ashby CR Jr (2001) Expression and acquisition of the conditioned place preference response to cocaine in rats is blocked by selective inhibitors of the enzyme N-acetylated-alpha-linked-acidic dipeptidase (NAALADASE). Synapse 41:22–28
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  17. Vyas CA, Rawls SM, Raffa RB, Shackman JG (2011) Glutamate and aspartate measurements in individual planaria by rapid capillary electrophoresis. J Pharmacol Toxicol Methods 63:199–222
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  19. Xi ZX, Li X, Peng XQ, Li J, Chun L, Gardner EL, Thomas AG, Slusher BS, Ashby CR Jr (2010a) Inhibition of NAALADase by 2-PMPA attenuates cocaine-induced relapse in rats: a NAAG-mGluR2/3-mediated mechanism. J Neurochem 112:564–576
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• 作者单位：1. Department of Pharmaceutical Sciences, Temple University Health Sciences Center, 3307 North Broad Street, Philadelphia, PA 19140, USA2. Center for Substance Abuse Research, Temple University, Philadelphia, PA 19140, USA
• 刊物类别：Biomedical and Life Sciences
• 刊物主题：Life Sciences
  Biochemistry
  Analytical Chemistry
  Biochemical Engineering
  Life Sciences
  Proteomics
  Neurobiology
  
• 出版者：Springer Wien
• ISSN：1438-2199

文摘

Glutamate carboxypeptidase II (GCPII) inhibitors are promising anti-glutamatergic and anti-addictive agents. We hypothesized that a GCPII inhibitor 2 (phosphonomethyl) pentanedioic acid (2-PMPA) would display anti-stereotypical activity in planarians. Experiments revealed that 2-PMPA displayed no overt behavioral activity by itself but attenuated stereotypical counts (C-shape hyperkinesias) elicited by four compounds (2-PMPA rank order potency: glutamate > NMDA > pilocarpine > cocaine). These data suggest GCPII inhibitors display broad-spectrum efficacy against behavioral activity produced by glutamatergic and non-glutamatergic compounds in an invertebrate assay.