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This study evaluates the reproducibility of the quantification of metabotropic glutamate receptor type 5 (mGluR5) densities in rats using the PET radiotracer [11C]ABP688 and pharmacokinetic models that are based on an input function, which is derived from a reference tissue. Seven rats underwent dynamic PET scans (60 min) after bolus injection of [11C]ABP688. Kinetic analyses included: binding potential...
We report on the pharmacological, behavioral, and neurochemical characterization of a novel dual norepinephrine (NE)/dopamine (DA) transporter inhibitor EB‐1020 (1R,5S)‐1‐(naphthalen‐2‐yl)‐3‐azabicyclo[3.1.0]hexane HCl). EB‐1020 preferentially inhibited monoamine reuptake in cloned cell lines transfected with human transporters with IC50 values of 6 and 38, respectively, for NE and DA transporters...
Inositol polyphosphate phosphatase 4 A (INPP4A), a phosphoinositides phosphatase, is highly expressed in the central nervous system and plays a role in glutamate excitotoxicity and cell proliferation. Our aim was to investigate the expression of INPP4A in patients with temporal lobe epilepsy (TLE) and in a rat model of epilepsy. We assessed the expression of INPP4A in the temporal neocortex from 20...
The density of the Imidazoline2 binding site (I2BS) has been shown to change in psychiatric conditions such as depression and addiction, along with neurodegenerative disorders such as Alzheimer's disease and Huntington's chorea. The presence of I2BS on glial cells and the possibility that they may in some way regulate glial fibrillary acidic protein has led to increased interest into the role of I...
Several classes of drugs bind to the dopamine transporter (DAT) with high affinity, but some are weaker positive reinforcers than cocaine, suggesting that affinity for and occupancy of the DAT is not the only determinant of a drug's reinforcing effectiveness. Other factors such as the rate of onset have been positively and strongly correlated with the reinforcing effects of DAT inhibitors in nonhuman...
Sleep disturbance has been reported to be one of the most frequent symptoms in patients suffered from severe pain. Benzodiazepines are effective and reduce anxiety in the hours after use, but the induced sleep tends to be less than ideal in quality, with increased Stages I–II and reduces Stages III–IV sleep. In the present study, we investigated sleep disturbance under a neuropathic pain‐like state...
This study examined the relationship between changes in GABA transmission and behavioral abnormalities after median nerve transection. Following unilateral median nerve transection, the percentage of GABA‐like immunoreactive neurons in the cuneate nucleus and that of GABAB receptor‐like immunoreactive neurons in the dorsal root ganglion in the injured side decreased and reached a nadir at 4 weeks...
Analysis of gait functions following spinal cord injury has been widely studied in rats, mice but limited in primates. This investigation was performed to quantitatively analyze the degree of functional recovery in bipedal locomotion in bonnet monkeys after induced spinal cord contusion. The degree of locomotor recovery was examined by measuring four gait variables, viz., tip of opposite foot (TOF),...
Rett syndrome (RTT) is a neurodevelopmental disability characterized by mutations in the X‐linked methyl‐CpG‐binding protein 2 located at the Xq28 region. The severity is modified in part by X chromosomal inactivation resulting in wide clinical variability. We hypothesized that the ability to perform the activities of daily living (ADL) is correlated with the density of vesicular acetylcholine transporters...
Although [11C]‐(+)‐PHNO has enabled quantification of the dopamine‐D3 receptor (D3R) in the human brain in vivo, its selectivity for the D3R is not sufficiently high to allow us to disregard its binding to the dopamine‐D2 receptor (D2R). We quantified the affinity of [11C]‐(+)‐PHNO for the D2R and D3R in the living primate brain. Two rhesus monkeys were examined on four occasions each, with [11C]‐(+)‐PHNO...
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