preparation-evaluation-99mtc-labeled-tridentate-chelates-for-pre

Preparation and Evaluation of <sup>99m</sup>Tc-labeled Tridentate Chelates for Pre-targeting Using Bioorthogonal Chemistry

Pre-targeting combined with bioorthogonal chemistry is emerging as an effective way to create new radiopharmaceuticals. Of the methods available, the ...

McMaster University

Traumatic diaphragmatic hernia (TDH) is generally a consequence of thoraco-abdominal trauma. Anaesthetic problems arise due to herniation of abdominal contents into the thoracic cavity causing diaphragmatic dysfunction, lung collapse, mediastinal shift and haemodynamic instability. Diagnosis depends on history, clinical signs and radiological investigations. Sometimes, it may be misdiagnosed as hydropneumothorax due to the presence of air and fluid in the viscera lying in the pleural cavity. We report a case of TDH mimicking hydropneumothorax on radiological investigations and subsequent surgical management, which led to serious complications.

Delayed traumatic diaphragmatic hernia mimicking hydropneumothorax.

Emerging perspectives in perioperative use of gabapentinoids.

A high yield synthesis of a novel, small molecule, bisphosphonate-modified trans-cyclooctene (TCO-BP, 2) that binds to regions of active bone metabolism and captures functionalized tetrazines in vivo, via the bioorthogonal inverse electron demand Diels-Alder (IEDDA) cycloaddition, was developed. A (99m)Tc-labeled derivative of 2 demonstrated selective localization to shoulder and knee joints in a biodistribution study in normal mice. Compound 2 reacted rapidly with a (177)Lu-labeled tetrazine in vitro, and pretargeting experiments in mice, using 2 and the (177)Lu-labeled tetrazine, yielded high activity concentrations in shoulder and knee joints, with minimal uptake in other tissues. Pretargeting experiments with 2 and a novel (99m)Tc-labeled tetrazine also produced high activity concentrations in the knees and shoulders. Critically, both radiolabeled tetrazines showed negligible uptake in the skeleton and joints when administered in the absence of 2. Compound 2 can be utilized to target functionalized tetrazines to bone and represents a convenient reagent to test novel tetrazines for use with in vivo bioorthogonal pretargeting strategies.

Article	Year
Delayed traumatic diaphragmatic hernia mimicking hydropneumothorax. Indian journal of anaesthesia\| PubMed ID: 24963185	2014
Emerging perspectives in perioperative use of gabapentinoids. Anesthesiology\| PubMed ID: 25050500	2014
A Bone-Seeking trans-Cyclooctene for Pretargeting and Bioorthogonal Chemistry: A Proof of Concept Study Using (99m)Tc- and (177)Lu-Labeled Tetrazines. Journal of medicinal chemistry\| PubMed ID: 27676258	2016

Zainab Ahmad

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