Literature DB >> 20614105

Serotonin2A receptor blockade and clinical effect in first-episode schizophrenia patients treated with quetiapine.

Hans Rasmussen1, Bjorn H Ebdrup, David Erritzoe, Bodil Aggernaes, Bob Oranje, Jan Kalbitzer, Lars H Pinborg, William F C Baaré, Claus Svarer, Henrik Lublin, Gitte M Knudsen, Birte Glenthoj.   

Abstract

RATIONALE: We have previously reported decreased frontal cortical serotonin2A receptor binding in 30 antipsychotic naïve first-episode schizophrenic patients and a relationship between this binding and positive psychotic symptoms. Until now, no longitudinal studies of serotonin2A receptor in first-episode antipsychotic-naïve schizophrenia patients have reported on the relationship between serotonin2A receptor occupancy and treatment effect after sustained treatment with a specific atypical antipsychotic compound.
OBJECTIVES: Here, we measured serotonin2A receptor occupancy with [(18)F]altanserin PET in 15 first-episode antipsychotic-naïve schizophrenia patients before and after 6 months of quetiapine treatment. Moreover, we investigated possible relationships between clinical efficacy, oral dose, and plasma levels of quetiapine
RESULTS: Significant nonlinear relationships were found between serotonin2A receptor occupancy, quetiapine dose, and plasma concentration. There was a modest effect on positive symptoms up until a serotonin2A receptor occupancy level of approximately 60%. A receptor occupancy level between 60% and 70% appeared to exert the optimal serotonin2A receptor related treatment effect on positive symptoms whereas no additional serotonin2A receptor associated treatment effect was obtained above a receptor occupancy of 70%.
CONCLUSIONS: Taken together, the data point to a therapeutic role of the serotonin2A receptor in the treatment of subgroups of patients with schizophrenia. Specifically, the study indicates a serotonin2A receptor associated therapeutic window on positive symptoms in responding patients in the range between 60% and 70% occupancy in antipsychotic-naïve first-episode schizophrenia. We speculate that non-responding patients need higher dopamine D(2) receptor blockade. Future studies with concurrent measurement of interactions with the dopamine system are, however, warranted to clarify this.

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Year:  2010        PMID: 20614105     DOI: 10.1007/s00213-010-1941-5

Source DB:  PubMed          Journal:  Psychopharmacology (Berl)        ISSN: 0033-3158            Impact factor:   4.530


  45 in total

Review 1.  Does fast dissociation from the dopamine d(2) receptor explain the action of atypical antipsychotics?: A new hypothesis.

Authors:  S Kapur; P Seeman
Journal:  Am J Psychiatry       Date:  2001-03       Impact factor: 18.112

2.  M-100907 (Aventis).

Authors:  T de Paulis
Journal:  Curr Opin Investig Drugs       Date:  2001-01

Review 3.  Consensus nomenclature for in vivo imaging of reversibly binding radioligands.

Authors:  Robert B Innis; Vincent J Cunningham; Jacques Delforge; Masahiro Fujita; Albert Gjedde; Roger N Gunn; James Holden; Sylvain Houle; Sung-Cheng Huang; Masanori Ichise; Hidehiro Iida; Hiroshi Ito; Yuichi Kimura; Robert A Koeppe; Gitte M Knudsen; Juhani Knuuti; Adriaan A Lammertsma; Marc Laruelle; Jean Logan; Ralph Paul Maguire; Mark A Mintun; Evan D Morris; Ramin Parsey; Julie C Price; Mark Slifstein; Vesna Sossi; Tetsuya Suhara; John R Votaw; Dean F Wong; Richard E Carson
Journal:  J Cereb Blood Flow Metab       Date:  2007-05-09       Impact factor: 6.200

4.  Serotonin 5-HT2 receptors in schizophrenia: a PET study using [18F]setoperone in neuroleptic-naive patients and normal subjects.

Authors:  R Lewis; S Kapur; C Jones; J DaSilva; G M Brown; A A Wilson; S Houle; R B Zipursky
Journal:  Am J Psychiatry       Date:  1999-01       Impact factor: 18.112

5.  MR-based automatic delineation of volumes of interest in human brain PET images using probability maps.

Authors:  Claus Svarer; Karine Madsen; Steen G Hasselbalch; Lars H Pinborg; Steven Haugbøl; Vibe G Frøkjaer; Søren Holm; Olaf B Paulson; Gitte M Knudsen
Journal:  Neuroimage       Date:  2004-12-09       Impact factor: 6.556

6.  [18F]altanserin binding to human 5HT2A receptors is unaltered after citalopram and pindolol challenge.

Authors:  Lars H Pinborg; Karen H Adams; Stig Yndgaard; Steen G Hasselbalch; Søren Holm; Heidi Kristiansen; Olaf B Paulson; Gitte M Knudsen
Journal:  J Cereb Blood Flow Metab       Date:  2004-09       Impact factor: 6.200

7.  Evidence for altered post-receptor modulation of the serotonin 2a receptor in schizophrenia.

Authors:  Brian Dean; Nicola Crossland; Simone Boer; Elizabeth Scarr
Journal:  Schizophr Res       Date:  2008-08-08       Impact factor: 4.939

8.  Quetiapine: an effective antipsychotic in first-episode schizophrenia despite only transiently high dopamine-2 receptor blockade.

Authors:  Sitra Tauscher-Wisniewski; Shitij Kapur; Johannes Tauscher; Corey Jones; Zafiris J Daskalakis; George Papatheodorou; Irvin Epstein; Bruce K Christensen; Robert B Zipursky
Journal:  J Clin Psychiatry       Date:  2002-11       Impact factor: 4.384

Review 9.  Clinical pharmacokinetics of atypical antipsychotics: a critical review of the relationship between plasma concentrations and clinical response.

Authors:  Massimo C Mauri; Lucia S Volonteri; Alessandro Colasanti; Alessio Fiorentini; Ilaria F De Gaspari; Silvio R Bareggi
Journal:  Clin Pharmacokinet       Date:  2007       Impact factor: 6.447

10.  Decreased frontal serotonin2A receptor binding in antipsychotic-naive patients with first-episode schizophrenia.

Authors:  Hans Rasmussen; David Erritzoe; Rune Andersen; Bjorn H Ebdrup; Bodil Aggernaes; Bob Oranje; Jan Kalbitzer; Jacob Madsen; Lars H Pinborg; William Baaré; Claus Svarer; Henrik Lublin; Gitte M Knudsen; Birte Glenthoj
Journal:  Arch Gen Psychiatry       Date:  2010-01
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  16 in total

1.  Serotonin revisited.

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Journal:  Psychopharmacology (Berl)       Date:  2010-12-22       Impact factor: 4.530

2.  Synthesis and imaging validation of [¹⁸F]MDL100907 enabled by Ni-mediated fluorination.

Authors:  Hong Ren; Hsiao-Ying Wey; Martin Strebl; Ramesh Neelamegam; Tobias Ritter; Jacob M Hooker
Journal:  ACS Chem Neurosci       Date:  2014-06-03       Impact factor: 4.418

3.  Serotonin 2A receptor agonist binding in the human brain with [¹¹C]Cimbi-36.

Authors:  Anders Ettrup; Sophie da Cunha-Bang; Brenda McMahon; Szabolcs Lehel; Agnete Dyssegaard; Anine W Skibsted; Louise M Jørgensen; Martin Hansen; Anders O Baandrup; Søren Bache; Claus Svarer; Jesper L Kristensen; Nic Gillings; Jacob Madsen; Gitte M Knudsen
Journal:  J Cereb Blood Flow Metab       Date:  2014-04-30       Impact factor: 6.200

4.  Structural brain correlates of sensorimotor gating in antipsychotic-naive men with first-episode schizophrenia.

Authors:  Trine Bjørg Hammer; Bob Oranje; Arnold Skimminge; Bodil Aggernæs; Bjørn H Ebdrup; Birte Glenthøj; William Baaré
Journal:  J Psychiatry Neurosci       Date:  2013-01       Impact factor: 6.186

5.  Interaction of mGlu2/3 agonism with clozapine and lurasidone to restore novel object recognition in subchronic phencyclidine-treated rats.

Authors:  Masakuni Horiguchi; Mei Huang; Herbert Y Meltzer
Journal:  Psychopharmacology (Berl)       Date:  2011-03-25       Impact factor: 4.530

6.  Role of the 5-HT₂A receptor in the locomotor hyperactivity produced by phenylalkylamine hallucinogens in mice.

Authors:  Adam L Halberstadt; Susan B Powell; Mark A Geyer
Journal:  Neuropharmacology       Date:  2013-01-29       Impact factor: 5.250

7.  Manganese-enhanced magnetic resonance imaging reveals increased DOI-induced brain activity in a mouse model of schizophrenia.

Authors:  Natalia V Malkova; Joseph J Gallagher; Collin Z Yu; Russell E Jacobs; Paul H Patterson
Journal:  Proc Natl Acad Sci U S A       Date:  2014-06-02       Impact factor: 11.205

Review 8.  Schizophrenia: synthetic strategies and recent advances in drug design.

Authors:  Maria Azmanova; Anaïs Pitto-Barry; Nicolas P E Barry
Journal:  Medchemcomm       Date:  2018-03-16       Impact factor: 3.597

Review 9.  5-HT radioligands for human brain imaging with PET and SPECT.

Authors:  Louise M Paterson; Birgitte R Kornum; David J Nutt; Victor W Pike; Gitte M Knudsen
Journal:  Med Res Rev       Date:  2011-06-14       Impact factor: 12.944

10.  Treatment Response in First-episode Schizophrenia.

Authors:  Rebecca Schennach; Michael Riedel; Richard Musil; Hans-Jürgen Möller
Journal:  Clin Psychopharmacol Neurosci       Date:  2012-08-31       Impact factor: 2.582

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