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

doi:10.1002/(SICI)1099-1344(1998090)41:9<843::AID-JLCR136>3.0.CO;2-H

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

Chemo-Pharmaceutical Sciences

Research output: Contribution to journal › Article › peer-review

18 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 language	English
Pages (from-to)	843-858
Number of pages	16
Journal	Journal of Labelled Compounds and Radiopharmaceuticals
Volume	41
Issue number	9
DOIs	https://doi.org/10.1002/(SICI)1099-1344(1998090)41:9<843::AID-JLCR136>3.0.CO;2-H
Publication status	Published - Sept 1998

All Science Journal Classification (ASJC) codes

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

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10.1002/(SICI)1099-1344(1998090)41:9<843::AID-JLCR136>3.0.CO;2-H

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Haradahira, T., Sasaki, S., Maeda, M., Kobayashi, K., Inoue, O., Tomita, U., Nishikawa, T., & Suzuki, K. (1998). Synthesis and brain distribution of carbon-11 labeled analogs of antagonists for the NMDA receptor coupled PCP-binding site. Journal of Labelled Compounds and Radiopharmaceuticals, 41(9), 843-858. https://doi.org/10.1002/(SICI)1099-1344(1998090)41:9<843::AID-JLCR136>3.0.CO;2-H

Haradahira, T, Sasaki, S, Maeda, M, Kobayashi, K, Inoue, O, Tomita, U, Nishikawa, T & Suzuki, K 1998, 'Synthesis and brain distribution of carbon-11 labeled analogs of antagonists for the NMDA receptor coupled PCP-binding site', Journal of Labelled Compounds and Radiopharmaceuticals, vol. 41, no. 9, pp. 843-858. https://doi.org/10.1002/(SICI)1099-1344(1998090)41:9<843::AID-JLCR136>3.0.CO;2-H

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

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.",

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

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AU - Haradahira, Terushi

AU - Sasaki, Sigeki

AU - Maeda, Minoru

AU - Kobayashi, Kaoru

AU - Inoue, Osamu

AU - Tomita, Urara

AU - Nishikawa, Toru

AU - Suzuki, Kazutoshi

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AB - 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.

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

Abstract

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