The arsenal of drugs for psychiatry has been difficult to renew for several decades. Many failures in therapeutic trials can be explained by poorly evaluated pharmacological properties, in terms of brain passage, target binding, and functional modulation. Positron emission tomography can provide pharmacokinetic and pharmacodynamic data that will help to better select candidate molecules for larger-scale clinical trials.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/acschemneuro.3c00036 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Fully Automated Production of ((()-1-Carboxy-5-(6-([F]fluoro)-2-methoxynicotinamido)pentyl)carbamoyl)-l-glutamic Acid ([F]JK-PSMA-7).
Pharmaceuticals (Basel)
January 2025
Forschungszentrum Jülich GmbH, Institute of Neuroscience and Medicine, Nuclear Chemistry (INM-5), Wilhelm-Johnen-Str., 52428 Jülich, Germany.
The radiotracer [F]JK-PSMA-7, a prostate cancer imaging agent for positron emission tomography (PET), was previously synthesized by indirect radiofluorination using an F-labeled active ester as a prosthetic group, which had to be isolated and purified before it could be linked to the pharmacologically active Lys-urea-Glu motif. Although this procedure could be automated on two-reactor modules like the GE TRACERLab FX2N (FXN) to afford the tracer in modest radiochemical yields (RCY) of 18-25%, it is unsuitable for cassette-based systems with a single reactor. To simplify implementation on an automated synthesis module, the radiosynthesis of [F]JK-PSMA-7 was devised as a one-pot, two-step reaction.
View Article and Find Full Text PDFUtilisation of the Innovative [18F]-Labelled Radiotracer [18F]-BIBD-071 Within HR+ Breast Cancer Xenograft Mouse Models.
Pharmaceuticals (Basel)
January 2025
Department of Nuclear Medicine, Beijing Tiantan Hospital, Capital Medical University, Beijing 100071, China.
Aromatase plays a crucial role in the conversion of androgens to oestrogens and is often overexpressed in hormone-dependent tumours, particularly breast cancer. [18F]BIBD-071, which has excellent binding affinity for aromatase and good pharmacokinetics, has potential for the diagnosis and treatment of aromatase-related diseases. The MCF-7 cell line, which is hormone receptor-positive (HR+), was used in the assessment of the novel [18F]-labelled radiotracer [18F]BIBD-071 via positron emission tomography (PET) imaging of an HR+ breast cancer xenograft model.
View Article and Find Full Text PDFRadiocobalt-Labeling of a Polypyridylamine Chelate Conjugated to GE11 for EGFR-Targeted Theranostics.
Molecules
January 2025
Department of Physics, Chemistry and Pharmacy, University of Southern Denmark, Campusvej 55, 5230 Odense M, Denmark.
The overexpression of the epidermal growth factor receptor (EGFR) in certain types of prostate cancers and glioblastoma makes it a promising target for targeted radioligand therapy. In this context, pairing an EGFR-targeting peptide with the emerging theranostic pair comprising the Auger electron emitter cobalt-58m (Co) and the Positron Emission Tomography-isotope cobalt-55 (Co) would be of great interest for creating novel radiopharmaceuticals for prostate cancer and glioblastoma theranostics. In this study, GE11 (YHWYGYTPQNVI) was investigated for its EGFR-targeting potential when conjugated using click chemistry to N1-((triazol-4-yl)methyl)-N1,N2,N2-tris(pyridin-2-ylmethyl)ethane-1,2-diamine (TZTPEN).
View Article and Find Full Text PDFRole of Ultrasonography in Monitoring Chemotherapeutic Effects on Primary Thyroid Lymphoma: A Single-Center Retrospective Study.
Medicina (Kaunas)
December 2024
Department of Ultrasound, Peking University Third Hospital, Beijing 100191, China.
In this study, we assessed the utility of ultrasonography in monitoring the chemotherapeutic effects on primary thyroid lymphoma (PTL). This retrospective analysis included 17 patients with PTL who received chemotherapy from 2012 to 2022. The sonographic features were examined pre- and post-treatment using ultrasound (US) to monitor the treatment response at the first to second, third to fourth, and end cycles of chemotherapy and follow-up, and progression-free survival (PFS) and overall survival (OS) were analyzed.
View Article and Find Full Text PDFImaging in Periprosthetic Joint Infection Diagnosis: A Comprehensive Review.
Microorganisms
December 2024
International Center for Limb Lengthening, Rubin Institute for Advanced Orthopedics, Sinai Hospital of Baltimore, Baltimore, MD 21215, USA.
Various imaging methods assist in diagnosing periprosthetic joint infection (PJI). These include radiological techniques such as radiography, computed tomography (CT), magnetic resonance imaging (MRI), and ultrasound (US); as well as advanced nuclear medicine techniques including bone scintigraphy (BS), anti-granulocyte antibody imaging (AGS), leukocyte scintigraphy (LS), and fluorodeoxyglucose positron emission tomography (FDG-PET and FDG-PET/CT). Each imaging technique and radiopharmaceutical has been extensively studied, with unique diagnostic accuracy, limitations, and benefits for PJI diagnosis.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!