Synthesis of N‐(¹¹C) methyl, N‐(methyl‐1 propyl), (chloro‐2 phenyl)‐1 isoquinoleine carboxamide‐3 (PK 11195): A new ligand for peripheral benzodiazepine receptors

Abstract

N-(llC) methyl, N-(methyl-1 propyl), (chloro-2 phenylj-1 isoquinoleine carboxamide-3 (PK 11195) o r ( l l C ) MPCI was synthetized in a short time (45 min) and high s p e c i f i c a c t i v i t y (769 Ci/mmol) 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 ( l k ) methyl iodide obtained from nuclear reaction 14N ( p , a ) 11C vit: 11CO2 and 11CH30H. The chemical p u r i t y of the end-product was checked, a f t e r HPLC p u r i f ication, by chemical ionisation mass spectrometry i n the para1 l e l synthesis of cold MPCI. The methylation, reversed phase HPLC p u r i f i c a t i o n , evaporation times were 10, 6 min respectively so t h a t s t e r i l e and i s o t o n i c i n j e c t a b l e solution o f ( l k ) MPCI ready f o r use may be obtained, i n l e s s t h a n 45 min a f t e r the end of nuclear bombardment.

Imaging microglial activation and glucose consumption in a mouse model of Alzheimer's disease

“…Radiosynthesis of [ 11 C]-(R)-PK11195 was accomplished by N-methylation using the method of Camsonne et al (1984) with slight modifications. 11 C was produced by the 14 N(p,α) 11 C nuclear reaction using the MC16 cyclotron (Scanditronix, Uppsala, Sweden) at the MPI for Neurological Research.…”

Neuroinflammation Extends Brain Tissue at Risk to Vital Peri-Infarct Tissue: A Double Tracer [11C]PK11195- and [18F]FDG-PET Study

“…11 C]PK11195 was accomplished by N-methylation using the method of Camsonne et al (1984) with slight modifications.…”

11C-AC-5216: A Novel PET Ligand for Peripheral Benzodiazepine Receptors in the Primate Brain

“…The increase in PBR density has thus been used as an indicator of neuronal damage and neurodenerative disorders, such as Alzheimer's disease (6)(7)(8)(9)(10)(11)(12). These findings have prompted the development of an imaging agent labeled with a radioisotope, which has made it possible to visualize the distribution of PBR in the animal brain, including the human brain (13)(14)(15)(16).…”