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Proceedings Paper

N-alkylated aminopyrazines for use as hydrophilic optical agents
Author(s): Amruta R. Poreddy; Bethel Asmelash; Karen P. Galen; Richard M. Fitch; Jeng-Jong Shieh; James M. Wilcox; Tasha M. Schoenstein; Jolette K. Wojdyla; Kimberly R. Gaston; John N. Freskos; William L. Neumann; Raghavan Rajagopalan; Hyo-Yang Ahn; James G. Kostelc; Martin P. Debreczeny; Kevin D. Belfield; Richard B. Dorshow
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Paper Abstract

Rapid assessment of glomerular filtration rate (GFR), which measures the amount of plasma filtered through the kidney within a given time, would greatly facilitate monitoring of renal function for patients at the bedside in the clinic. In our pursuit to develop exogenous fluorescent tracers for real-time monitoring of renal function by optical methods, N-alkylated aminopyrazine dyes and their hydrophilic conjugates based on poly (ethylene glycol) (PEG) were synthesized via reductive amination as the key step. Photophysical properties indicated a bathochromic shift on the order of 50 nm in both absorption and emission compared to naked aminopyrazines which could be very useful in enhancing both tissue penetration as well as easier detection methods. Structure-activity relationship (SAR) and pharmacokinetic (PK) studies, and the correlation of in vivo optical data with plasma PK for measurement of clearance (and hence GFR) are focus of the current investigation.

Paper Details

Date Published: 21 February 2009
PDF: 10 pages
Proc. SPIE 7190, Reporters, Markers, Dyes, Nanoparticles, and Molecular Probes for Biomedical Applications, 71900P (21 February 2009); doi: 10.1117/12.809287
Show Author Affiliations
Amruta R. Poreddy, Covidien Imaging Solutions (United States)
Bethel Asmelash, Covidien Imaging Solutions (United States)
Karen P. Galen, Covidien Imaging Solutions (United States)
Richard M. Fitch, Covidien Imaging Solutions (United States)
Jeng-Jong Shieh, Covidien Imaging Solutions (United States)
James M. Wilcox, Covidien Imaging Solutions (United States)
Tasha M. Schoenstein, Covidien Imaging Solutions (United States)
Jolette K. Wojdyla, Covidien Imaging Solutions (United States)
Kimberly R. Gaston, Covidien Imaging Solutions (United States)
John N. Freskos, Covidien Imaging Solutions (United States)
William L. Neumann, Covidien Imaging Solutions (United States)
Raghavan Rajagopalan, Covidien Imaging Solutions (United States)
Hyo-Yang Ahn, Univ. of Central Florida (United States)
James G. Kostelc, Covidien Imaging Solutions (United States)
Martin P. Debreczeny, Covidien Imaging Solutions (United States)
Kevin D. Belfield, Univ. of Central Florida (United States)
Richard B. Dorshow, Covidien Imaging Solutions (United States)


Published in SPIE Proceedings Vol. 7190:
Reporters, Markers, Dyes, Nanoparticles, and Molecular Probes for Biomedical Applications
Samuel Achilefu; Ramesh Raghavachari, Editor(s)

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