Area measurements taken from receptor autoradiograms were employed to estimate the size of striatal kainate lesions and the amount of shrinkage in deafferented projection areas. There was no significant difference in the size of substantia nigra (SN) on the denervated side as compared to the intact side one week and one month after unilateral striatal lesions. Although there was no change in the size of globus pallidus (GP) on the lesioned side one week after the lesion, there was a 17% shrinkage one month after the lesion. At 3-4 months after the lesion, the amount of shrinkage was 19% in SN and 16% in GP.
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http://dx.doi.org/10.1016/0304-3940(84)90035-1 | DOI Listing |
ACS Chem Neurosci
October 2023
Center for Radiopharmaceutical Sciences ETH-PSI-USZ, Institute of Pharmaceutical Sciences ETH, Vladimir-Prelog-Weg 4, 8093 Zurich, Switzerland.
The cannabinoid type 2 receptor (CB2) has been implicated in a variety of central and peripheral inflammatory diseases, prompting significant interest in the development of CB2-targeted diagnostic and therapeutic agents. A validated positron emission tomography (PET) radioligand for imaging CB2 in the living human brain as well as in peripheral tissues is currently lacking. As part of our research program, we have recently identified the trisubstituted pyridine, [F]RoSMA-18-d, which proved to be highly suitable for and mapping of CB2 in rodents.
View Article and Find Full Text PDFActa Pharm Sin B
January 2023
Department of Radiology, Division of Nuclear Medicine and Molecular Imaging Massachusetts General Hospital and Harvard Medical School, Boston, MA 02114, USA.
There is an accumulating body of evidence implicating the muscarinic acetylcholine receptor 4 (M) in schizophrenia and dementia with Lewy bodies, however, a clinically validated M positron emission tomography (PET) radioligand is currently lacking. As such, the aim of this study was to develop a suitable M PET ligand that allows the non-invasive visualization of M in the brain. Structure-activity relationship studies of pyrazol-4-yl-pyridine derivates led to the discovery of target compound a subtype-selective positive allosteric modulator (PAM).
View Article and Find Full Text PDFRes Sq
January 2023
Department of Radiology, Division of Nuclear Medicine and Molecular Imaging Massachusetts General Hospital and Harvard Medical School, 55 Fruit Street, Boston, MA 02114, USA.
GluN2B subunit-containing -methyl-d-aspartate (NMDA) receptors have been implicated in various neurological disorders. Nonetheless, a validated fluorine-18 labeled positron emission tomography (PET) ligand for GluN2B imaging in the living human brain is currently lacking. As part of our PET ligand development program, we have recently reported on the preclinical evaluation of [F]OF-NB1 - a GluN2B PET ligand with promising attributes for potential clinical translation.
View Article and Find Full Text PDFNucl Med Biol
October 2022
Amsterdam UMC, VU University Medical Center, Radiology & Nuclear Medicine (Amsterdam Cardiovascular Sciences), de Boelelaan 1085c, Amsterdam, the Netherlands.
The transforming growth factor β (TGFβ) pathway plays a complex role in cancer biology, being involved in both tumour suppression as well as promotion. Overactive TGFβ signalling has been linked to multiple diseases, including cancer, pulmonary arterial hypertension, and fibrosis. One of the key meditators within this pathway is the TGFβ type I receptor, also termed activin receptor-like kinase 5 (ALK5).
View Article and Find Full Text PDFNucl Med Biol
June 2022
Laboratory of Bioanalysis and Molecular Imaging, Graduate School of Pharmaceutical Sciences, Hokkaido University, Sapporo, Hokkaido, Japan; Global Station for Biosurfaces and Drug Discovery, Global Institution for Collaborative Research and Education (GI-CoRE), Hokkaido University, Sapporo, Hokkaido, Japan. Electronic address:
Introduction: Hypoxia is common in solid tumors and creates an immunosuppressive environment that leads to resistance to immunotherapy, such as an anti-programmed death receptor-1 (PD-1) therapy. It has been suggested that anti-PD-1 therapy may reduce tumor hypoxia by remodeling the tumor vasculature; however, it is unclear how anti-PD-1 therapy reduces hypoxia over time. Therefore, we investigated the relationship between hypoxia and immune activation by anti-PD-1 therapy in murine cancer models.
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