The iodination of alpha-bungarotoxin and the reactivity of iodinated derivatives towards nicotinic acetylcholine receptor are described. 125I2- and 125I-alpha-bungarotoxin can be resolved, but the latter was not separated from unreacted alpha-bungarotoxin. A study of the reactivities of the various forms of the toxin towards nicotinic acetylcholine receptor indicated that di-iodination had modified its reactivity. The 125I2-form bound with a slower rate constant than alpha-bungarotoxin to the receptor. 125I-alpha-bungarotoxin showed no modification of reactivity towards the receptor. Apart from the A280, two methods for calibrating 125I-alpha-bungarotoxin are described. They may be employed in the presence of other proteins. The first of these is an immunological assay using the complex formed between toxin and antitoxin antibodies. The second is a dilution assay, where competition between iodinated and noniodinated toxins for binding sites on nicotinic acetylcholine receptor is exploited.
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http://dx.doi.org/10.1515/bchm2.1980.361.2.1517 | DOI Listing |
J Biomech
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Department of Orthodontics, Beijing Stomatological Hospital, Capital Medical University, Capital Medical University School of Stomatology, Beijing 100050, China.
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View Article and Find Full Text PDFInt J Parasitol Drugs Drug Resist
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Applied Bioscience Graduate Program, Faculty of Science, University of Ontario Institute of Technology, 2000 Simcoe Street North, Oshawa, ON, L1G 0C5, Canada. Electronic address:
The acetylcholine-gated chloride channel (ACC) family in parasitic nematodes represents a promising target for anthelmintic drug development. Levamisole, a widely known and utilized cholinergic agonist, has been used for decades to address many types of parasitic infections by targeting nematode nicotinic acetylcholine receptors (nAChRs) in nematodes. In this study, we report the synthesis and pharmacological evaluation of eight levamisole derivatives, five of which are novel, on the H.
View Article and Find Full Text PDFTaiwan J Obstet Gynecol
March 2025
Department of Medical Research, MacKay Memorial Hospital, Taipei, Taiwan.
Objective: A case of prenatal diagnosis of familial 15q13.2q13.3 microdeletion is presented.
View Article and Find Full Text PDFJ Med Chem
March 2025
Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Unversitetsparken 2, DK-2100 Copenhagen Ø, Denmark.
A plethora of agonists and competitive antagonists have been developed to explore the therapeutic potential in neuronal nicotinic acetylcholine receptors (nAChRs). Based on equilibrium and kinetic [H]epibatidine binding studies, we report that the kinetic fingerprints of [H]epibatidine at five heteromeric αβ nAChRs and of seven classical agonists at α4β2 and α3β4 nAChRs differ substantially. While this diversity depends on both the agonist and receptor subtype, the overall pattern of kinetic determinants emerging from this profiling is complex.
View Article and Find Full Text PDFJ Cachexia Sarcopenia Muscle
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Department of Anesthesiology, Critical Care and Pain Medicine, Massachusetts General Hospital, Shriners Hospital for Children, and Harvard Medical School, Boston, Massachusetts, USA.
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