Literature DB >> 12392747

SB-656104-A: a novel 5-HT(7) receptor antagonist with improved in vivo properties.

Ian T Forbes1, Sara Douglas, Andrew D Gribble, Robert J Ife, Andrew P Lightfoot, Ashley E Garner, Graham J Riley, Phillip Jeffrey, Alexander J Stevens, Tania O Stean, David R Thomas.   

Abstract

A focused SAR study around the previously reported selective 5-HT(7) receptor antagonist, SB-269970-A has resulted in the identification of a structurally related analogue having an improved pharmacokinetic profile. Replacement of the phenolic group in SB-269970-A with an indole moiety, and replacement of the piperidinyl 4-methyl group with a heterocyclic ring system proved to be the key changes leading to the identification of SB-656104-A.

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Year:  2002        PMID： 12392747     DOI： 10.1016/s0960-894x(02)00690-x

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


  15 in total

Review 1.  Serotonin 5-HT7 receptor agents: Structure-activity relationships and potential therapeutic applications in central nervous system disorders.

Authors:  Marcello Leopoldo; Enza Lacivita; Francesco Berardi; Roberto Perrone; Peter B Hedlund
Journal:  Pharmacol Ther       Date:  2010-10-20       Impact factor: 12.310

2.  Modulation of 5-HT7 receptor: effect on object recognition performances in mice.

Authors:  Thomas Freret; Eleni Paizanis; Gregory Beaudet; Andreia Gusmao-Montaigne; Gerald Nee; François Dauphin; Valentine Bouet; Michel Boulouard
Journal:  Psychopharmacology (Berl)       Date:  2013-08-31       Impact factor: 4.530

3.  Structural insight into the serotonin (5-HT) receptor family by molecular docking, molecular dynamics simulation and systems pharmacology analysis.

Authors:  Yuan-Qiang Wang; Wei-Wei Lin; Nan Wu; Si-Yi Wang; Mao-Zi Chen; Zhi-Hua Lin; Xiang-Qun Xie; Zhi-Wei Feng
Journal:  Acta Pharmacol Sin       Date:  2019-02-27       Impact factor: 6.150

4.  Sensitization of restraint-induced corticosterone secretion after chronic restraint in rats: involvement of 5-HT₇ receptors.

Authors:  Brenda B García-Iglesias; María E Mendoza-Garrido; Gabriel Gutiérrez-Ospina; Claudia Rangel-Barajas; Martha Noyola-Díaz; José A Terrón
Journal:  Neuropharmacology       Date:  2013-03-28       Impact factor: 5.250

5.  The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors.

Authors:  Stephen P H Alexander; Helen E Benson; Elena Faccenda; Adam J Pawson; Joanna L Sharman; Michael Spedding; John A Peters; Anthony J Harmar
Journal:  Br J Pharmacol       Date:  2013-12       Impact factor: 8.739

6.  Increase of capsaicin-induced trigeminal Fos-like immunoreactivity by 5-HT(7) receptors.

Authors:  Esther Martínez-García; Marcello Leopoldo; Enza Lacivita; José A Terrón
Journal:  Headache       Date:  2011 Nov-Dec       Impact factor: 5.887

7.  Systemic morphine produce antinociception mediated by spinal 5-HT7, but not 5-HT1A and 5-HT2 receptors in the spinal cord.

Authors:  A Dogrul; M Seyrek
Journal:  Br J Pharmacol       Date:  2006-08-14       Impact factor: 8.739

8.  Amide conjugates of ketoprofen and indole as inhibitors of Gli1-mediated transcription in the Hedgehog pathway.

Authors:  Neeraj Mahindroo; Michele C Connelly; Chandanamali Punchihewa; Lei Yang; Bing Yan; Naoaki Fujii
Journal:  Bioorg Med Chem       Date:  2010-05-07       Impact factor: 3.641

9.  Evidence for the involvement of central 5-HT7 receptors in the micturition reflex in anaesthetized female rats.

Authors:  Kate E Read; Gareth J Sanger; Andrew G Ramage
Journal:  Br J Pharmacol       Date:  2003-07-29       Impact factor: 8.739

10.  SB-656104-A, a novel selective 5-HT7 receptor antagonist, modulates REM sleep in rats.

Authors:  David R Thomas; Sergio Melotto; Mario Massagrande; Andrew D Gribble; Phillip Jeffrey; Alexander J Stevens; Nigel J Deeks; Peter J Eddershaw; Susan H Fenwick; Graham Riley; Tania Stean; Claire M Scott; Matthew J Hill; Derek N Middlemiss; Jim J Hagan; Gary W Price; Ian T Forbes
Journal:  Br J Pharmacol       Date:  2003-06       Impact factor: 8.739
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