N-Alkylated aminopyrazines for use as hydrophilic optical agents

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

Research output: Chapter in Book/Report/Conference proceedingConference contribution

2 Scopus citations

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, Nalkylated 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.

Original languageEnglish (US)
Title of host publicationReporters, Markers, Dyes, Nanoparticles, and Molecular Probes for Biomedical Applications
DOIs
StatePublished - Jun 15 2009
Externally publishedYes
EventReporters, Markers, Dyes, Nanoparticles, and Molecular Probes for Biomedical Applications - San Jose, CA, United States
Duration: Jan 26 2009Jan 29 2009

Publication series

NameProgress in Biomedical Optics and Imaging - Proceedings of SPIE
Volume7190
ISSN (Print)1605-7422

Other

OtherReporters, Markers, Dyes, Nanoparticles, and Molecular Probes for Biomedical Applications
Country/TerritoryUnited States
CitySan Jose, CA
Period1/26/091/29/09

All Science Journal Classification (ASJC) codes

  • Electronic, Optical and Magnetic Materials
  • Biomaterials
  • Atomic and Molecular Physics, and Optics
  • Radiology Nuclear Medicine and imaging

Keywords

  • Fluorescence
  • GFR
  • Optical monitoring
  • PEG
  • Pyrazine
  • Reductive amination
  • Renal clearnce.
  • Renal function

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