title: Glutamate carboxypeptidase II (GCPII) inhibitor displays anti-glutamate and anti-cocaine effects in an invertebrate assay.
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.
authors.affiliation: Department of Pharmaceutical Sciences, Temple University Health Sciences Center, 3307 North Broad Street, Philadelphia, PA 19140, USA.
authors.forename: Chris
authors.initials: C
authors.lastname: Tallarida
authors.forename: Kevin
authors.initials: K
authors.lastname: Song
authors.forename: Robert B
authors.initials: RB
authors.lastname: Raffa
authors.forename: Scott M
authors.initials: SM
authors.lastname: Rawls
mesh_terms: D000818:Animals; D003042:Cocaine / Q000494:pharmacology / Q000633:toxicity; D043425:Glutamate Carboxypeptidase II / Q000037:antagonists & inhibitors* / Q000378:metabolism; D018698:Glutamic Acid / Q000494:pharmacology / Q000633:toxicity; D023421:Models, Animal; D016202:N-Methylaspartate / Q000494:pharmacology / Q000633:toxicity; D009943:Organophosphorus Compounds / Q000494:pharmacology*; D010862:Pilocarpine / Q000494:pharmacology / Q000633:toxicity; D010932:Planarians; D013239:Stereotyped Behavior / Q000187:drug effects*
chemical_list: C402107:2-(phosphonomethyl)pentanedioic acid; D009943:Organophosphorus Compounds; D010862:Pilocarpine; D018698:Glutamic Acid; D016202:N-Methylaspartate; D043425:Glutamate Carboxypeptidase II; D003042:Cocaine