Literature DB >> 11086728

Novel 2,3,4,5-tetrahydro-1H-3-benzazepines with high affinity and selectivity for the dopamine D3 receptor.

N E Austin1, K Y Avenell, I Boyfield, C L Branch, M S Hadley, P Jeffrey, C N Johnson, G J Macdonald, D J Nash, G J Riley, A B Smith, G Stemp, K M Thewlis, A K Vong, M Wood.   

Abstract

Starting from the dopamine D3 receptor antagonist SB-277011 1, a series of 2,3,4,5-tetrahydro-1H-3-benzazepines has been identified with high affinity for the dopamine D3 receptor and selectivity over the D2 receptor. The 3-acetamido-2-fluorocinnamide derivative 20 gave high D3 receptor affinity (pKi 8.4) with 130-fold selectivity over the 2, receptor.

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Year:  2000        PMID： 11086728     DOI： 10.1016/s0960-894x(00)00505-9

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


  3 in total

Review 1.  The role of central dopamine D3 receptors in drug addiction: a review of pharmacological evidence.

Authors:  Christian A Heidbreder; Eliot L Gardner; Zheng-Xiong Xi; Panayotis K Thanos; Manolo Mugnaini; Jim J Hagan; Charles R Ashby
Journal:  Brain Res Brain Res Rev       Date:  2005-07

2.  Chronic ethanol self-administration in macaques shifts dopamine feedback inhibition to predominantly D2 receptors in nucleus accumbens core.

Authors:  Cody A Siciliano; Erin S Calipari; Jordan T Yorgason; Yolanda Mateo; Christa M Helms; David M Lovinger; Kathleen A Grant; Sara R Jones
Journal:  Drug Alcohol Depend       Date:  2015-11-10       Impact factor: 4.492

3.  Studies of new fused benzazepine as selective dopamine D3 receptor antagonists using 3D-QSAR, molecular docking and molecular dynamics.

Authors:  Jing Liu; Yan Li; Shuwei Zhang; Zhengtao Xiao; Chunzhi Ai
Journal:  Int J Mol Sci       Date:  2011-02-18       Impact factor: 5.923
  3 in total

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