title: Preliminary experience with an ampakine (CX516) as a single agent for the treatment of schizophrenia: a case series.
abstract: We used L-(quinoxalin-6-ylcarbonyl)piperidine (CX516) (a modulator of the alpha-amino-3-hydroxy-5-methyl-4-isoxasole propionic acid (AMPA) receptor) as a sole agent in a double blind placebo-controlled design in a small series of patients with schizophrenia who were partially refractory to treatment with traditional neuroleptics. The study entailed weekly increments in doses of CX516, from 300 mg tid for week 1 up to 900 mg tid on week 4. Patients were followed with clinical ratings, neuropsychological testing, and were monitored for adverse events. Four patients received 2 to 4 weeks of CX516, two received placebo and two withdrew during the placebo phase. Adverse events associated with drug administration were transient and included leukopenia in one patient and elevation in liver enzymes in another. No clear improvement in psychosis or in cognition was observed over the course of the study. CX516 at the doses tested did not appear to yield dramatic effects as a sole agent, but inference from this study is limited.
authors.affiliation: Intramural Research Program, Clinical Brain Disorders Branch, National Institute of Mental Health, Building 10, Room 4S235, Bethesda, MD 20892, USA. marenco@intra.nimh.nih.gov
authors.forename: Stefano
authors.initials: S
authors.lastname: Marenco
authors.forename: Michael F
authors.initials: MF
authors.lastname: Egan
authors.forename: Terry E
authors.initials: TE
authors.lastname: Goldberg
authors.forename: Michael B
authors.initials: MB
authors.lastname: Knable
authors.forename: Robert K
authors.initials: RK
authors.lastname: McClure
authors.forename: Georg
authors.initials: G
authors.lastname: Winterer
authors.forename: Daniel R
authors.initials: DR
authors.lastname: Weinberger
mesh_terms: D000328:Adult; D014150:Antipsychotic Agents / Q000009:adverse effects / Q000627:therapeutic use*; D004149:Dioxoles / Q000009:adverse effects / Q000627:therapeutic use*; D004311:Double-Blind Method; D005260:Female; D006801:Humans; D008297:Male; D008875:Middle Aged; D010880:Piperidines / Q000009:adverse effects / Q000627:therapeutic use*; D011618:Psychotic Disorders / Q000188:drug therapy*; D012559:Schizophrenia / Q000188:drug therapy*
chemical_list: C097396:1-(quinoxalin-6-ylcarbonyl)piperidine; D014150:Antipsychotic Agents; D004149:Dioxoles; D010880:Piperidines