[18F]GBR13119 (1-[(4-[18F]fluorophenyl)-(phenyl)methoxy]ethyl-4-(3-phenylpropyl) piperazine) has been prepared in no carrier added form by a four-step synthesis from [18F]fluoride. Isolated yields are 7-10% (uncorrected) in a synthesis time of 120 min. The product is obtained in high specific activity (greater than 1000 Ci/mmol) and high radiochemical purity (greater than 99%) without chromatographic purification. Small amounts of chemical impurity, identified as the nitro-substituted analog by independent synthesis, can be removed by HPLC. [18F]GBR13119 is proposed as a new radiotracer for the presynaptic dopamine uptake system.
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http://dx.doi.org/10.1016/0883-2889(88)90015-9 | DOI Listing |
Exp Neurol
January 2025
Department of Physiology and Pathophysiology, School of Basic Medical Sciences, Xi'an Jiaotong University Health Science Center, Xi'an 710061, China. Electronic address:
Depression is one of the most common non-motor symptoms in Parkinson's disease (PD) and the hyperactivity of the lateral habenula (LHb) may contribute to depression. The present study was performed to investigate the effects and mechanisms of group I metabotropic glutamate receptors (mGluRs) in the LHb on PD-related depressive-like behaviors. Unilateral 6-hydroxydopamine lesions of the substantia nigra pars compacta (SNc) were used to establish the PD rat model.
View Article and Find Full Text PDFMov Disord
January 2025
Department of Neurology, Vanderbilt University Medical Center, Nashville, Tennessee, USA.
Background: Central synucleinopathies, including Parkinson's disease (PD), dementia with Lewy bodies (DLB), and multiple system atrophy (MSA), involve alpha-synuclein accumulation and dopaminergic cell loss in the substantia nigra (SN) and locus coeruleus (LC). Pure autonomic failure (PAF), a peripheral synucleinopathy, often precedes central synucleinopathies.
Objectives: To assess early brain involvement in PAF using neuromelanin-sensitive magnetic resonance imaging (NM-MRI) and fluorodopa-positron emission tomography (FDOPA-PET), and to determine whether PAF patients with a high likelihood ratio (LR) for conversion to a central synucleinopathy exhibit reduced NM-MRI contrast in the LC and SN compared with controls and low-LR patients.
NPJ Parkinsons Dis
January 2025
Interfaculty Institute of Biochemistry, University of Tübingen, Tübingen, Germany.
The dysfunction of dopaminergic (DA) neurons is central to Parkinson's disease. Distinct synaptic vesicle (SV) populations, differing in neurotransmitter content (dopamine vs. glutamate), may vary due to differences in trafficking and exocytosis.
View Article and Find Full Text PDFInt J Mol Sci
December 2024
Section of Affective Disorders, Department of Psychiatry, Jagiellonian University Medical College, Kopernika 21a, 31-501 Kraków, Poland.
Lumateperone is a novel antipsychotic recently approved for the treatment of schizophrenia. Its unique pharmacological profile includes modulation of serotonergic, dopaminergic, and glutamatergic neurotransmission, differentiating it from other second-generation antipsychotics. This paper explores the pharmacological features and clinical potential of lumateperone across neuropsychiatric conditions.
View Article and Find Full Text PDFInt J Biol Macromol
January 2025
Department of Pharmaceutical and Pharmacological Sciences, University of Padova, Padova, Italy. Electronic address:
α-Synuclein (Syn) is an intrinsically disordered protein, abundant in presynaptic neurons. It is a constituent of the Lewis Body inclusions as amyloid fibrils, in Parkinson's disease patients. It populates an ensemble of conformations and floats between the free random coil and the membrane-bound α-helical species.
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