Synthesis and brain distribution of carbon-11 labeled analogs of antagonists for the NMDA receptor coupled PCP-binding site

Terushi Haradahira, Sigeki Sasaki, Minoru Maeda, Kaoru Kobayashi, Osamu Inoue, Urara Tomita, Toru Nishikawa, Kazutoshi Suzuki

Research output: Contribution to journalArticle

17 Citations (Scopus)

Abstract

Two phencyclidine (PCP) analogs, 3 and 4, and one thienylcyclohexylpiperidine (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.

Original languageEnglish
Pages (from-to)843-858
Number of pages16
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Volume41
Issue number9
DOIs
Publication statusPublished - Sep 1 1998

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tenocyclidine
N-Methyl-D-Aspartate Receptors
Brain
Carbon
Binding Sites
Phencyclidine
Positrons
Ion Channels
Electrons
Molecules

All Science Journal Classification (ASJC) codes

  • Analytical Chemistry
  • Biochemistry
  • Radiology Nuclear Medicine and imaging
  • Drug Discovery
  • Spectroscopy
  • Organic Chemistry

Cite this

Synthesis and brain distribution of carbon-11 labeled analogs of antagonists for the NMDA receptor coupled PCP-binding site. / Haradahira, Terushi; Sasaki, Sigeki; Maeda, Minoru; Kobayashi, Kaoru; Inoue, Osamu; Tomita, Urara; Nishikawa, Toru; Suzuki, Kazutoshi.

In: Journal of Labelled Compounds and Radiopharmaceuticals, Vol. 41, No. 9, 01.09.1998, p. 843-858.

Research output: Contribution to journalArticle

Haradahira, Terushi ; Sasaki, Sigeki ; Maeda, Minoru ; Kobayashi, Kaoru ; Inoue, Osamu ; Tomita, Urara ; Nishikawa, Toru ; Suzuki, Kazutoshi. / Synthesis and brain distribution of carbon-11 labeled analogs of antagonists for the NMDA receptor coupled PCP-binding site. In: Journal of Labelled Compounds and Radiopharmaceuticals. 1998 ; Vol. 41, No. 9. pp. 843-858.
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