| Title : Radiosynthesis and mouse brain distribution studies of [11C] CP-126,998: a PET ligand for in vivo study of acetylcholinesterase - Musachio_2002_Nucl.Med.Biol_29_547 |
| Author(s) : Musachio JL , Flesher JE , Scheffel UA , Rauseo P , Hilton J , Mathews WB , Ravert HT , Dannals RF , Frost JJ |
| Ref : Nucl Med Biol , 29 :547 , 2002 |
|
Abstract :
The selective, reversible acetylcholinesterase inhibitor 5,7-Dihydro-7-methyl-3- [2-[1-(phenylmethyl]-4-piperidinyl]ethyl]-6H-pyrrolo[3,2-f]-1,2-benzisoxazol3-6-o ne (CP-126,998) was labeled with C-11 iodomethane via base-promoted alkylation of the lactam nitrogen. [11C] CP-126,998 was synthesized in good radiochemical yield (13-29% non-decay corrected) and high specific radioactivity (177-418 GBq/micromol). In vivo mouse biodistribution studies reveal [11C] CP-126,998 to localize preferentially in striatal tissue, a region known to be rich in acetylcholinesterase. Competitive blocking studies using a variety of acetylcholinesterase inhibitors (diisopropylfluorophosphate, tacrine, CP-118,954) verified the specificity of the PET radiotracer for brain acetylcholinesterase. |
| PubMedSearch : Musachio_2002_Nucl.Med.Biol_29_547 |
| PubMedID: 12088724 |
| Inhibitor | Icopezil |
Musachio JL, Flesher JE, Scheffel UA, Rauseo P, Hilton J, Mathews WB, Ravert HT, Dannals RF, Frost JJ (2002)
Radiosynthesis and mouse brain distribution studies of [11C] CP-126,998: a PET ligand for in vivo study of acetylcholinesterase
Nucl Med Biol
29 :547
Musachio JL, Flesher JE, Scheffel UA, Rauseo P, Hilton J, Mathews WB, Ravert HT, Dannals RF, Frost JJ (2002)
Nucl Med Biol
29 :547