A sensitive and simple radioreceptor assay system for measuring methionine(met)-enkephalin-like substance in human cerebrospinal fluid (CSF) was developed using a particulate fraction of rat brain as a receptor preparation and [3H]dihydromorphine as a radiolabeled ligand in the presence of 1 mM ethylenediamine tetracetate (EDTA) and 2 mM magnesium acetate. Metenkephalin-like substance was purified from CSF by the combination of Sephadex G-10 and SP-Sephadex (H+) column chromatographies to be free of sodium and large molecular weight substance such as beta-endorphin. The assays were carried out on samples obtained from normal subjects and patients with the disease of the brain or pituitary by lumbar or ventricular puncture. Mean level in samples obtained from normal subjects by lumbar puncture was 2.6 +/- 1.0 pmoles/ml.
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http://dx.doi.org/10.1016/0304-3959(80)90029-9 | DOI Listing |
Eur J Nucl Med Mol Imaging
January 2025
Institute of Radiation Medicine, Fudan University, Xietu Road 2094, Shanghai, 200032, China.
Objectives: Mesothelin (MSLN) is an antigen that is overexpressed in various cancers, and its interaction with tumor-associated cancer antigen 125 plays a multifaceted role in tumor metastasis. The serum MSLN expression level can be detected using enzyme-linked immunosorbent assay; however, non-invasive visualization of its expression at the tumor site is currently lacking. Therefore, the aim of this study was to develop a molecular probe for imaging MSLN expression through positron emission tomography (PET).
View Article and Find Full Text PDFBioorg Med Chem Lett
January 2025
Contineum Therapeutics, 3565 General Atomics Court, Suite 200, San Diego, CA 92121, United States.
Novel kappa opioid receptor (KOR) agonists that preferentially activate G-protein signaling versus β-arrestin-2 recruitment are described. Starting from a literature-reported phenol-containing diphenethylamine KOR agonist, structure-activity relationship (SAR) studies revealed replacement of the phenol with various non-hydroxylated bicyclic heteroaromatics led to tertiary diarylethylamines which retained KOR agonist activity and improved metabolic stability in human liver microsomes. Further optimizations produced compound 39, a potent activator of G-protein signaling (GTPγS EC = 14 nM, 83 % E) that did not elicit a β-arrestin-2 recruitment functional response (E < 10 %).
View Article and Find Full Text PDFObesity is a global health crisis, with its prevalence particularly severe in the United States, where over 42% of adults are classified as obese. Obesity is driven by complex molecular and tissue-level mechanisms that remain poorly understood. Among these, angiogenesis-primarily mediated by vascular endothelial growth factor (VEGF-A)-is critical for adipose tissue expansion but presents unique challenges for therapeutic targeting due to its intricate regulation.
View Article and Find Full Text PDFACS Omega
December 2024
Heidelberg University, Medical Faculty Mannheim, Biomedical Chemistry, Theodor-Kutzer-Ufer 1-3, 68167 Mannheim, Germany.
By possibly bridging the gap between 2D cell assays and applications, tumor cell spheroid cultures offer promising avenues for advancing innovation in nuclear medicine. Regarding the evaluation of therapeutic radioligands, tumor cell spheroids have been successfully used to assess the therapeutic efficacy against human tumors. However, studies employing spheroids for testing diagnostic tracers are missing.
View Article and Find Full Text PDFBioorg Med Chem
February 2025
Department of Radiology, Washington University School of Medicine, St. Louis, MO 63110, United States. Electronic address:
The purinergic P2X ligand-gated ion channel 7 receptor (P2X7R) plays a critical role in various inflammatory processes and other diseases. Fast determination of compounds P2X7R binding potency and discovery of a promise PET radiotracer for imaging P2X7R require a P2X7R suitable radioligand for radioactive competitive binding assay. Herein, we designed and synthesized thirteen new P2X7R ligands and determined the in vitro binding potency.
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