Detail lodine-123 labelled Z-(R,R)-IQNP: a potential radioligand for visualization of M1 and M2 muscarinic acetylcholine receptors in Alzheimer's disease (Short communication in European Journal of Nuclear Medicine Vol. 26, No. 11) Bibliografi Author: Bergstrom, Kim A. ; Halldin, Christer ; Savonen, Aki ; Okubo, Yoshiro ; Hiltunen, Jukka ; Nobuhara, Kenji ; Swahn, Carl-Gunnar ; Karlsson, Per ; McPherson, Dan ; Knapp, Furn F. [Jr.] ; Larsson, Stig ; Schnell, Per-Olof ; Farde, Lars Topik: Short communication; Z-(R; R)-IQNP; Muscarinic acetylcholine receptors; Brain; Single-photon emission tomography Bahasa: (EN )    Edisi: Nov 1999     Penerbit: Springer-Verlag Berlin Heidelberg     Tempat Terbit: Heidelberg    Tahun Terbit: 1999     Jenis: Article - diterbitkan di jurnal ilmiah internasional Fulltext: article_14.pdf (675.1KB; 0 download) [Informasi yang berkaitan dengan koleksi ini di internet] Abstract Z-(R)-1-Azabicyclo[2.2.2]oct-3-yl (R)-a-hydroxy-a-(1-iodo-1-propen-3-yl)-a-phenylacetate (Z-IQNP) has high affinity to the M1 and M2 muscarinic acetylcho¬line receptor (mAChR) subtypes according to previous in vitro and in vivo studies in rats. In the present study iodine-123 labelled Z-IQNP was prepared for in vivo single-photon emission tomography (SPET) studies in cynomolgus monkeys. SPET studies with Z-[123I]IQNP demonstrated high accumulation in monkey brain (>5% of injected dose at 70 min p.i.) and marked accumulation in brain regions such as the thalamus, the neocortex, the striatum and the cerebellum. Pretreatment with the non-selective mAChR antagonist scopolamine (0.2 mg/kg) inhibited Z-[123I]IQNP binding in all these regions. The percentage of unchanged Z-[123I]IQNP measured in plas¬ma was less than 10% at 10 min after injection, which may be due to rapid hydrolysis, as has been demonstrat¬ed previously with the E-isomer of IQNP. Z-[123I]IQNP showed higher uptake in M2-rich regions, compared with previously obtained results with E-[123I]IQNP. In conclu¬sion, the radioactivity distribution from Z-[I23I]IQNP in monkey brain indicates that Z-[123I]IQNP binds to the M1 and M2-rich areas and provides a high signal for specific binding, and is thus a potential ligand for mAChR imaging with SPET. Opini Anda Klik untuk menuliskan opini Anda tentang koleksi ini! Lihat Sejarah Pengadaan  Konversi Metadata   Kembali

Copyright © 2006, 2007 Unika Atma Jaya, all rights reserved