Synthesis and biological evaluation of novel 123I-labeled 4-(4-iodophenyl)butanoyl-l-prolyl-(2S)-pyrrolidines for imaging聽prolyl oligopeptidase in聽vivo
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- 作者：Annukka Kallinena ; annukka.kallinen@helsinki.fi" class="auth_mail ; annukka.kallinen@ansto.gov.au" class="auth_mail ; Boyan Todorova ; Roope Kallionpä ; ä ; b ; Susanne Bä ; ckc ; Mirkka Sarparantaa ; Mari Rakid ; Juan A. Garcí ; a-Horsmanc ; Kim A. Bergströ ; md ; e ; Erik A.A. Wallé ; nb ; Pekka T. Mä ; nnistö ; c ; Anu J. Airaksinena ; anu.airaksinen@helsinki.fi" class="auth_mail
- 关键词：123I-radiotracer ; Prolyl oligopeptidase ; Biodistribution ; Inflammation
- 刊名：European Journal of Medicinal Chemistry
- 出版年：22 May 2014
- 年：2014
- 卷：79
- 期：Complete
- 页码：436-445
- 全文大小：1264 K
文摘
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123I-labeled prolylpyrrolidines were synthesized for imaging prolyl oligopeptidase.
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The binding affinities of 123I-radiotracers were at low nanomolar range.
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4-(4-[123I]iodophenyl)butanoyl-l-prolyl-2(S)-cyanopyrrolidine was evaluated in vivo.
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The binding of evaluated tracer was prolyl oligopeptidase specific.
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The tracer was further evaluated in two animal models of inflammation.