Literature DB >> 23259035

Synthesis and in vitro evaluation of oxindole derivatives as potential radioligands for 5-HT(7) receptor imaging with PET.

Matthias M Herth, Balázs Volk, Katalin Pallagi, Lasse Kofoed Bech, Ferenc A Antoni, Gitte M Knudsen, Jesper L Kristensen.   

Abstract

The most recently discovered serotonin (5-HT) receptor subtype, 5-HT(7), is considered to be associated with several CNS disorders. Noninvasive in vivo positron emission tomography (PET) studies of cerebral 5-HT(7) receptors could provide a significant advance in the understanding of the neurobiology and eventual dysfunctions of the 5-HT(7) receptor. To date, no appropriate 5-HT(7) receptor PET ligand has been developed. Here, we modified known 5-HT(7) selective phenylpiperazinyl-butyloxindole derivatives so that they may be labeled either with carbon-11 or fluorine-18. A set of potential 5-HT(7) ligands for PET molecular imaging was successfully synthesized. Two compounds (10 and 14) were tested against a range of targets. Both compounds display a promising in vitro profile with respect to PET imaging of the 5-HT(7) receptor in thalamic regions.

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Year:  2012        PMID： 23259035      PMCID： PMC3526961          DOI： 10.1021/cn3001137

Source DB:  PubMed          Journal:  ACS Chem Neurosci        ISSN： 1948-7193            Impact factor:   4.418


  29 in total

1.  [3H]-SB-269970 radiolabels 5-HT7 receptors in rodent, pig and primate brain tissues.

Authors:  D R Thomas; P J Atkinson; P G Hastie; J C Roberts; D N Middlemiss; G W Price
Journal:  Neuropharmacology       Date:  2002-01       Impact factor: 5.250

2.  Looking for a 5-HT7 radiotracer for positron emission tomography.

Authors:  Julien Andriès; Laëtitia Lemoine; Alice Mouchel-Blaisot; Sandrine Tang; Mathieu Verdurand; Didier Le Bars; Luc Zimmer; Thierry Billard
Journal:  Bioorg Med Chem Lett       Date:  2010-04-24       Impact factor: 2.823

3.  Risperidone irreversibly binds to and inactivates the h5-HT7 serotonin receptor.

Authors:  Carol Smith; Tariq Rahman; Nicole Toohey; Joseph Mazurkiewicz; Katharine Herrick-Davis; Milt Teitler
Journal:  Mol Pharmacol       Date:  2006-07-26       Impact factor: 4.436

4.  Autoradiographic localization of 5-HT1A receptors in the post-mortem human brain using [3H]WAY-100635 and [11C]way-100635.

Authors:  H Hall; C Lundkvist; C Halldin; L Farde; V W Pike; J A McCarron; A Fletcher; I A Cliffe; T Barf; H Wikström; G Sedvall
Journal:  Brain Res       Date:  1997-01-16       Impact factor: 3.252

5.  Autoradiographic analysis of alpha 1-noradrenergic receptors in the human brain postmortem. Effect of suicide.

Authors:  R Gross-Isseroff; K A Dillon; S J Fieldust; A Biegon
Journal:  Arch Gen Psychiatry       Date:  1990-11

6.  Novel potent neuropeptide Y Y5 receptor antagonists: synthesis and structure-activity relationships of phenylpiperazine derivatives.

Authors:  Toshiyuki Takahashi; Aya Sakuraba; Tomoko Hirohashi; Takunobu Shibata; Masaaki Hirose; Yuji Haga; Katsumasa Nonoshita; Tetsuya Kanno; Junko Ito; Hisashi Iwaasa; Akio Kanatani; Takehiro Fukami; Nagaaki Sato
Journal:  Bioorg Med Chem       Date:  2006-08-17       Impact factor: 3.641

7.  Autoradiographic localization of 5-HT(2A) receptors in the human brain using [(3)H]M100907 and [(11)C]M100907.

Authors:  H Hall; L Farde; C Halldin; C Lundkvist; G Sedvall
Journal:  Synapse       Date:  2000-12-15       Impact factor: 2.562

8.  Pharmacological profile of lurasidone, a novel antipsychotic agent with potent 5-hydroxytryptamine 7 (5-HT7) and 5-HT1A receptor activity.

Authors:  Tadashi Ishibashi; Tomoko Horisawa; Kumiko Tokuda; Takeo Ishiyama; Masaaki Ogasa; Rie Tagashira; Kenji Matsumoto; Hiroyuki Nishikawa; Yoko Ueda; Satoko Toma; Hitomi Oki; Norihiko Tanno; Ikutaro Saji; Akira Ito; Yukihiro Ohno; Mitsutaka Nakamura
Journal:  J Pharmacol Exp Ther       Date:  2010-04-19       Impact factor: 4.030

Review 9.  State of art in 11C labelled radiotracers synthesis.

Authors:  M Allard; E Fouquet; D James; M Szlosek-Pinaud
Journal:  Curr Med Chem       Date:  2008       Impact factor: 4.530

10.  Decarbonylation of multi-substituted [18F]benzaldehydes for modelling syntheses of 18F-labelled aromatic amino acids.

Authors:  Bin Shen; Dirk Löffler; Klaus-Peter Zeller; Michael Ubele; Gerald Reischl; Hans-Jürgen Machulla
Journal:  Appl Radiat Isot       Date:  2007-06-26       Impact factor: 1.513
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  4 in total

Review 1.  PET tracers for serotonin receptors and their applications.

Authors:  J S Dileep Kumar; J John Mann
Journal:  Cent Nerv Syst Agents Med Chem       Date:  2014

Review 2.  Radiotracers for the Central Serotoninergic System.

Authors:  Reynald Mangeant; Emmanuelle Dubost; Thomas Cailly; Valérie Collot
Journal:  Pharmaceuticals (Basel)       Date:  2022-05-03

3.  Autoradiographic Evaluation of [(18)F]FECUMI-101, a High Affinity 5-HT1AR Ligand in Human Brain.

Authors:  J S Dileep Kumar; Mark D Underwood; Norman R Simpson; Suham A Kassir; Jaya Prabhakaran; Vattoly J Majo; Mihran J Bakalian; Ramin V Parsey; J John Mann; Victoria Arango
Journal:  ACS Med Chem Lett       Date:  2016-03-13       Impact factor: 4.345

4.  Synthesis and in vivo evaluation of [(18)F]2-(4-(4-(2-(2-fluoroethoxy)phenyl)piperazin-1-yl)butyl)-4-methyl-1,2,4-triazine-3,5(2H,4H)-dione ([(18)F]FECUMI-101) as an imaging probe for 5-HT1A receptor agonist in nonhuman primates.

Authors:  Vattoly J Majo; Matthew S Milak; Jaya Prabhakaran; Pratap Mali; Lyudmila Savenkova; Norman R Simpson; J John Mann; Ramin V Parsey; J S Dileep Kumar
Journal:  Bioorg Med Chem       Date:  2013-06-12       Impact factor: 3.641
  4 in total

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