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Synthesis of a radiolabeled charged melatonin receptor ligand
Author(s) -
Chu GuoHua,
Li PuiKai
Publication year - 1998
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/(sici)1099-1344(199805)41:5<435::aid-jlcr97>3.0.co;2-l
Subject(s) - chemistry , melatonin , ligand (biochemistry) , receptor , iodide , melatonin receptor , yield (engineering) , chemical synthesis , stereochemistry , medicinal chemistry , combinatorial chemistry , biochemistry , in vitro , organic chemistry , medicine , materials science , metallurgy
The synthesis of the first permanently charged melatonin receptor ligand: N‐[2‐(2‐trimethyl‐ammoniumethyleneoxy‐7‐methoxynaphthyl)ethyl]propionamide iodide ( 2a , TMEPI) and its carbon‐14 analog ( 2b , 14 C‐TMEPI) are described. The ligands can serve as tools to elucidate the mechanism of melatonin receptor regulation. Both compounds 2a and 2b are synthesized in 8 steps. The radiochemical yield and purity of 2b are 99.6 and 99.8% respectively, with specific radioactivity of 7.6 mCi/mmol. © 1998 John Wiley & Sons, Ltd.