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Synthesis and brain distribution of carbon‐11 labeled analogs of antagonists for the NMDA receptor coupled PCP‐binding site
Author(s) -
Haradahira Terushi,
Sasaki Sigeki,
Maeda Minoru,
Kobayashi Kaoru,
Inoue Osamu,
Tomita Urara,
Nishikawa Toru,
Suzuki Kazutoshi
Publication year - 1998
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/(sici)1099-1344(1998090)41:9<843::aid-jlcr136>3.0.co;2-h
Subject(s) - phencyclidine , chemistry , nmda receptor , piperidine , stereochemistry , binding site , receptor , in vivo , sigma receptor , in vitro , biophysics , biochemistry , microbiology and biotechnology , biology
Two phencyclidine (PCP) analogs, 3 and 4 , and one thienylcyclohexyl‐piperidine (TCP) analog, (±) 6 , were labeled with positron emitter carbon‐11. These compounds displayed higher in vitro binding affinities than PCP itself for the PCP‐binding site located inside the ion channel on the N‐methyl‐D‐aspartate (NMDA) receptors. Brain distribution studies in mice showed different uptake characteristics between the PCP and TCP analogs, indicating their different in vivo interactions with the brain components including the PCP‐binding site probably due to the different physicochemical properties of the molecules. © 1998 John Wiley & Sons, Ltd.