Pyruvaldehyde Bis Research Articles

A remote system for the synthesis of copper-62 labeled Cu(PTSM)

The construction and performance of a remote system is described for the synthesis of 62Cu-labeled pyruvaldehyde bis( N 4-methylthiosemicarbazonato)copper(II), [ 62Cu]Cu(PTSM), a positron-emitting radiopharmaceutical for perfusion imaging. The remote system allows the shielded synthesis and purification of tracer using the 2 M HCl eluate of high-level (10–18 GBq) 62Zn/ 62Cu radionuclide generator system. The remote system allows the [ 62Cu]Cu(PTSM) synthesis to be performed in under 8 min with ca 40% E.O.S. radiochemical yield and >98% radiochemical purity.

Assessment of regional myocardial and renal blood flow with copper-PTSM and positron emission tomography.

We recently demonstrated in isolated, perfused hearts that radiolabeled pyruvaldehyde bis(N4-methylthiosemicarbazonato)copper(II) (Cu-PTSM) is well extracted throughout a range of conditions including ischemia, hypoxia, and hyperemia. Once extracted, binding of radioactivity by the isolated heart was essentially irreversible, giving this tracer microspherelike qualities. Because Cu-PTSM can be readily prepared with the generator-produced positron-emitting copper 62 and other gamma- or positron-emitting copper radionuclides, we evaluated its usefulness for measuring regional myocardial and renal blood flow in vivo in intact dogs at rest, after ischemia, or after coronary hyperemia was induced by intravenous administration of dipyridamole. After intravenous administration of radiolabeled Cu-PTSM, the tracer cleared rapidly from the blood. Myocardial uptake of single photon-emitting 67Cu-labeled Cu-PTSM was measured directly in myocardial samples 15 minutes after tracer administration, and it increased proportionally with blood flow throughout the flow range (estimated concomitantly with radiolabeled microspheres) of 0.0-6.0 ml/g/min (n = 340 samples from 17 dogs, r = 0.99, Ycopper radioactivity = 85Xmicrosphere flow -7 chi 2 + 17). Renal uptake of radiolabeled Cu-PTSM was also proportional to blood flow. Positron emission tomography was performed in four intact dogs after intravenous administration of 64Cu-labeled Cu-PTSM (19% positron decay, t1/2 = 12.8 hours). High-quality images of heart and kidney were obtained. Accordingly, radiolabeled Cu-PTSM should be a useful, generator-produced tracer for estimating regional myocardial and renal blood flow with positron emission tomography.

Structural characterization of a metal-based perfusion tracer: Copper(II) pyruvaldehyde bis ( N4-methylthiosemicarbazone)

Copper(II) pyruvaldehyde bis( N 4-methylthiosemicarbazone), Cu(PTSM), has been obtained as a dark red crystalline solid from EtOH-DMSO solvent mixture and structurally characterized by x-ray crystallography. The molecule possesses the expected pseudo-square planar N 2S 2 metal coordination sphere; however, the copper center also interacts through its axial coordination site with the sulfur atom of an adjacent Cu(PTSM) molecule in the crystal lattice. The structure of this compound is compared with the structures of other metal complexes that have been proposed in the nuclear medicine literature as perfusion tracers.

A potential copper radiopharmaceutical for imaging the heart and brain: Copper-labeled pyruvaldehyde bis( N4-methylthiosemicarbazone)

An investigation of the biodistribution of lipophilic copper-64 (half-life = 12.7 h) compounds has been initiated in order to screen potential tracers that could be used to measure regional cerebral and/or myocardial blood flow when labeled with generator-produced 62Cu. The 64Cu complex of pyruvaldehyde bis( N 4-methylthiosemicarbazone), [ 64Cu]Cu-PTSM, was prepared and found to be lipophlic (octanol/saline partition coefficient, log p = 1.97 ± 0.03). Biodistribution studies following i.v. injection of [ 64Cu]Cu-PTSM into rats show tracer uptake by the brain and heart. At 1, 5, and 15 min post-injection 3.3, 3.0 and 2.7% of the injected dose was found in the brain. Corresponding brain to blood ratios (per gram) were 3.2, 3.6 and 4.0 respectively. Heart to blood ratios of 7.6, 7.6 and 7.3 were observed at these same time points.

Stability of pyruvaldehyde bis(thiosemicarbazone) and its copper chelate

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTStability of pyruvaldehyde bis(thiosemicarbazone) and its copper chelateJames G. Cappuccino, Masao Arakawa, and M. Earl BalisCite this: J. Med. Chem. 1968, 11, 2, 399–401Publication Date (Print):March 1, 1968Publication History Published online1 May 2002Published inissue 1 March 1968https://doi.org/10.1021/jm00308a062RIGHTS & PERMISSIONSArticle Views81Altmetric-Citations2LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InReddit PDF (375 KB) Get e-Alerts Get e-Alerts