Premium
Synthesis and in vivo evaluation (PIG) of CP‐643,051, the N ‐[ 11 C]methyl analogue of the NK 1 receptor antagonist CP‐122,721
Author(s) -
Bender D.,
Smith D. F.,
Marthi K.,
Gjedde A.
Publication year - 2001
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.25804401100
Subject(s) - chemistry , in vivo , methyl iodide , methylation , receptor , antagonist , ligand (biochemistry) , receptor antagonist , radiosynthesis , yield (engineering) , iodide , chemical synthesis , stereochemistry , in vitro , medicinal chemistry , biochemistry , organic chemistry , gene , microbiology and biotechnology , biology , materials science , metallurgy
The goal of this study was the synthesis and in vivo evaluation of a non‐peptide compound for studying the NK 1 receptor by PET. An N ‐methyl analogue of CP‐122, 721, i. e. CP‐643, 051 was chosen. Radiolabelling was achieved by N ‐methylation of CP‐122, 721 with [ 11 C]methyl iodide. Within 38 min (from EOB) 680 MBq of [ 11 C]CP‐643, 051 (radiochemical yield: 7%, purity >95%, S.A.: 37 GBq/μmol) was produced. Brain uptake and distribution were studied in anaesthetised pig. In conclusion, due to low brain uptake the compound is not a suitable ligand for studying the NK 1 receptor in vivo .