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Synthesis, characterization, and in vivo disposition of iodinatable polyethylene glycol derivatives: Differences in vivo as a function of chain length
Author(s) -
Larwood David J.,
Szoka Francis C.
Publication year - 1984
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580210703
Subject(s) - polyethylene glycol , chemistry , in vivo , peg ratio , histamine , diamine , peg 400 , organic chemistry , polymer chemistry , nuclear chemistry , pharmacology , medicine , microbiology and biotechnology , finance , economics , biology
A series of iodinatable water soluble polyethylene glycol (PEG) derivatives were prepared for use as model hydrophilic drugs. Polyethylene glycol diamine 6000 was coupled to methyl p ‐hydroxybenzimidate, and PEG 1900‐ and PEG 5000‐monomethyl ethers were coupled to tyramine and histamine. The derivatives underwent facile iodination with the chloramine‐T reaction and were stable under a wide range of conditions. The larger derivatives showed rapid renal clearance, but the 1900 MW compounds underwent significant clearance via the bile.