当前位置： SCI文献检索 > NUCLEAR MEDICINE AND BIOLOGY期刊下所有文献 > Synthesis and evaluation of (11)C-labeled (S)-N-[[1-(2-phenylethyl) pyrrolidin-2-yl]methyl]-3-methylthiobenzamide as a PET 5-HT(1A) receptor ligand.

Synthesis and evaluation of (11)C-labeled (S)-N-[[1-(2-phenylethyl) pyrrolidin-2-yl]methyl]-3-methylthiobenzamide as a PET 5-HT(1A) receptor ligand.

Abstract：

:We prepared 5-HT(1A) receptor ligands (S)-N-[[1-(2-phenylethyl)pyrrolidin-2-yl]methyl]-3-[11C]methylthiobenzamide ([11C](S)-PPMMB) (Ki = 4.3 nM) and the less active [(11)C](R)-PPMMB (Ki = 160 nM) by reduction of the disulfide dimer and subsequent [(11)C]methylation of demethyl (S)- and (R)-PPMMB, respectively. Both radioligands showed similar brain distribution in mice with relatively higher affinity for the hippocampus being rich in 5-HT(1A) receptors than for other brain regions. Uptake of [(11)C](S)-PPMMB was not reduced by carrier-loading nor by pretreatment with 5-HT(1A) receptor ligands. [(11)C](S)-PPMMB is therefore not a suitable radioligand for mapping 5-HT(1A) receptors using positron emission tomography.

journal_name

Nucl Med Biol

journal_title

Nuclear medicine and biology

authors

Fujio M,Nagata S,Kawamura K,Sugiyama N,Tanaka H,Uno K,Ishiwata K

doi

10.1016/s0969-8051(02)00305-0

keywords:

subject

Has Abstract

pub_date

2002-08-01 00:00:00

pages

657-63

issue

6

eissn

0969-8051

issn

1872-9614

pii

S0969805102003050

journal_volume

29

pub_type

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