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The aim of this study was to explore the potential of a new selective dopamine transporter (DAT) compound as a radioligand for positron emission tomography (PET) examination of DAT in the human brain. The high affinity DAT compound N-(3-iodoprop-2 E-enyl)-2beta-carbomethoxy-3beta-(4-methylphenyl)nortropane (PE2I) was radiolabelled by the O-methylation approach and the binding was characterised by PET in cynomolgus monkeys and a healthy man. Metabolite levels in plasma were measured by gradient high-performance liquid chromatography. O-methylation of the corresponding free acid precursor with [(11)C]methyl triflate gave high radiochemical yield (80%) and specific radioactivity (55 GBq/ microM). [(11)C]PE2I binding in cynomolgus monkeys was nine times higher in the striatum than in the cerebellum at peak equilibrium, which appeared 55-65 min after injection. Displacement and pretreatment measurements using unlabelled beta-CIT, GBR 12909, cocaine, citalopram and maprotiline confirmed that [(11)C]PE2I binds selectively to DAT. In a preliminary study in one human subject the radioactivity ratios of the striatum and substantia nigra to the cerebellum were 10 and 1.8, respectively, at peak equilibrium, which appeared at 40-50 min and 20 min, respectively, after injection. The fraction of the total radioactivity in monkey and human plasma representing unchanged [(11)C]PE2I was 15-20% at 40 min after injection. The present characterisation of binding in monkey and man suggests that [(11)C]PE2I is a suitable PET radioligand for quantitative regional examination of DAT in man.

ObjectiveThe objective of this study was to evaluate the effect of oral appliance (OA) treatment on cognitive functions in patients with obstructive sleep apnea (OSA).Materials and methodsIn a prospective study, 50 male patients with verified moderate-to-severe OSA received an OA with mandibular advancement. The cognitive functions assessed included working memory, vigilance, executive functioning, and mental pace, measured before as well as after 6 months of treatment. Somnography was used to measure physiological treatment effects. Forty-three patients completed the 6-month follow-up study.ResultsAll domains of cognitive functioning measured improved after 6 months of treatment with an OA (P <; 0.001). The apnea/hypopnea- and oxygen desaturation-indices decreased significantly after treatment (P <; 0.01). An obvious treatment response was reached in 60% of the patients, and 54% of the patients had recovered ie, had normalized breathing during sleep.ConclusionOA with mandibular advancement is a treatment modality for the physiological symptoms of OSA, and may have a positive impact on cognitive functions, after only 6 months of treatment.

IntroductionThe goals with modern treatment of schizophrenia are to achieve remission of clinical symptoms, prevent relapse, and to restore the patients’ functions.Objectives/aimsThe objective of this study was to investigate the impact of treatment with the partial dopamine agonist aripiprazole on functions, measured as time spent for work or studies, in patients with schizophrenia or schizoaffective disorder.MethodsRetrospective data on employment and study activities were collected for all patients between 18–65 years with schizophrenia or schizoaffective disorder at an open care psychosis clinic in Sweden (n = 104). Possible impact of treatment with aripiprazole and of other variables, such as age, gender, and disease severity, was analysed.ResultsAmong patients who worked or studied at Day of admission (n = 36), the probability of maintaining or increasing time for work or studies was significantly higher in patients treated with aripiprazole compared with patients who were not (88% versus 53%; P = 0.020). This difference remained significant after controlling for severity of symptoms, age and sex. A secondary analysis, including all patients (independent of work or study status at Day of admission) also showed a significant difference in favour of aripiprazole (53% versus 26%, P = 0.005).ConclusionsThe results indicate that patients treated with aripiprazole (monotherapy or add-on) have higher probability of maintaining functional capacity. A plausible explanation might be aripiprazole's favourable effect on cognitive functions.Disclosure of interestThe authors have not supplied their declaration of competing interest.