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Synthesis of N‐( 11 C) methyl, N‐(methyl‐1 propyl), (chloro‐2 phenyl)‐1 isoquinoleine carboxamide‐3 (PK 11195): A new ligand for peripheral benzodiazepine receptors
Author(s) -
Camsonne R,
Crouzel C,
Comar D,
Mazière M,
Prenant C,
Sastre J,
Moulin Ma,
Syrota A
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.2580211012
Subject(s) - chemistry , methyl iodide , desmethyl , carboxamide , ligand (biochemistry) , high performance liquid chromatography , chemical synthesis , receptor , lead compound , stereochemistry , medicinal chemistry , chromatography , in vitro , biochemistry , metabolite
N‐( 11 c) methyl, N‐(methyl‐1 propyl), (chloro‐2 phenyl)‐1 isoquinoleine carboxamide‐3 (PK 11195) or ( 11 C) MPCI was synthetized in a short time (45 min) and high specific activity (769 Ci/mmo 1) for the positron emission tomography of peripheral benzodiazepine receptors in heart, kidney and brain. The precursor used was the N‐desmethyl MPCI (PCI). The radioactive reagent was the ( 11 C) methyl iodide obtained from nuclear reaction 14 N (p, α) 11 C via 11 CO 2 and 11 CH 3 OH. The chemical purity of the end‐product was checked, after HPLC purification, by chemical ionisation mass spectrometry in the parallel synthesis of cold MPCI. The methylation, reversed phase HPLC purification, evaporation times were 10, 6 min respectively so that sterile and isotonic injectable solution of ( 11 C) MPCI ready for use may be obtained, in less than 45 min after the end of nuclear bombardment.