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

Authors :: Tallarida C
Song K
Raffa RB
Rawls SM
Source :: Amino acids [Amino Acids] 2012 Jun; Vol. 42 (6), pp. 2521-4. Date of Electronic Publication: 2011 Aug 18.
Publication Year :: 2012
Abstract: 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.

Subjects :: Animals
Cocaine pharmacology
Cocaine toxicity
Glutamate Carboxypeptidase II metabolism
Glutamic Acid pharmacology
Glutamic Acid toxicity
Models, Animal
N-Methylaspartate pharmacology
N-Methylaspartate toxicity
Pilocarpine pharmacology
Pilocarpine toxicity
Planarians
Glutamate Carboxypeptidase II antagonists & inhibitors
Organophosphorus Compounds pharmacology
Stereotyped Behavior drug effects

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