Literature DB >> 15225707

Synthesis and radioiodination of selective ligands for the dopamine D3 receptor subtype.

Carsten Hocke1, Olaf Prante, Stefan Löber, Harald Hübner, Peter Gmeiner, Torsten Kuwert.   

Abstract

Starting from FAUC 365, a series of iodine substituted heteroaryl carboxamides has been synthesized revealing high affinity and selectivity for the dopamine D3 receptor. Binding data showed a 15-560-fold selectivity for the dopamine D3 over D2. A 2,3-dichloro substitution pattern on the phenylpiperazine moiety led to the highest subtype selectivity, whereas the 2-methoxy substituted compounds showed superior D3 affinity. Suitable precursors were radioiodinated with high radiochemical yields (53-85%) leading to potential imaging agents for the D3 receptor by SPET.

Entities:  

Mesh：

Substances：

Year:  2004        PMID： 15225707     DOI： 10.1016/j.bmcl.2004.05.052

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  5 in total

1.  Subtype selectivity of dopamine receptor ligands: insights from structure and ligand-based methods.

Authors:  Qi Wang; Robert H Mach; Robert R Luedtke; David E Reichert
Journal:  J Chem Inf Model       Date:  2010-10-11       Impact factor: 4.956

2.  Parallel synthesis of a multi-substituted benzo[b]furan library.

Authors:  Chul-Hee Cho; Benjamin Neuenswander; Gerald H Lushington; Richard C Larock
Journal:  J Comb Chem       Date:  2008-10-21

3.  N-(4-(4-(2,3-dichloro- or 2-methoxyphenyl)piperazin-1-yl)butyl)heterobiarylcarboxamides with functionalized linking chains as high affinity and enantioselective D3 receptor antagonists.

Authors:  Amy Hauck Newman; Peter Grundt; George Cyriac; Jeffrey R Deschamps; Michelle Taylor; Rakesh Kumar; David Ho; Robert R Luedtke
Journal:  J Med Chem       Date:  2009-04-23       Impact factor: 7.446

4.  Synthesis of multi-functionalized benzofurans through the condensation of ninhydrin and phenols using SSA as a recyclable heterogeneous acid catalyst.

Authors:  Ashis Kundu; Animesh Pramanik
Journal:  Mol Divers       Date:  2016-02-01       Impact factor: 2.943

5.  Design, synthesis, and structure-activity relationship studies of a series of [4-(4-carboxamidobutyl)]-1-arylpiperazines: insights into structural features contributing to dopamine D3 versus D2 receptor subtype selectivity.

Authors:  Subramaniam Ananthan; Surendra K Saini; Guangyan Zhou; Judith V Hobrath; Indira Padmalayam; Ling Zhai; J Robert Bostwick; Tamara Antonio; Maarten E A Reith; Shea McDowell; Eunie Cho; Leah McAleer; Michelle Taylor; Robert R Luedtke
Journal:  J Med Chem       Date:  2014-08-15       Impact factor: 7.446
  5 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.