Literature DB >> 20222157

Fenfluramine-induced serotonin release decreases [11C]AZ10419369 binding to 5-HT1B-receptors in the primate brain.

S J Finnema1, A Varrone, T J Hwang, B Gulyás, M E Pierson, C Halldin, L Farde.   

Abstract

The need for positron emission tomography (PET)-radioligands that are sensitive to changes in endogenous serotonin (5-HT) levels in brain is recognized in experimental and clinical psychiatric research. We recently developed the novel PET radioligand [(11)C]AZ10419369 that is highly selective for the 5-HT(1B) receptor. In this PET-study in three cynomolgus monkeys, we examined the sensitivity of [(11)C]AZ10419369 to altered endogenous 5-HT levels. Fenfluramine-induced 5-HT release decreased radioligand binding in a dose-dependent fashion with a regional average of 27% after 1 mg/kg and 50% after 5 mg/kg. This preliminary study supports that [(11)C]AZ10419369 is sensitive to endogenous 5-HT levels in vivo and may serve as a tool to examine the pathophysiology and treatment of major psychiatric disorders.

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Year:  2010        PMID： 20222157     DOI： 10.1002/syn.20780

Source DB:  PubMed          Journal:  Synapse        ISSN： 0887-4476            Impact factor:   2.562


  20 in total

1.  Confirmation of fenfluramine effect on 5-HT(1B) receptor binding of [(11)C]AZ10419369 using an equilibrium approach.

Authors:  Sjoerd J Finnema; Andrea Varrone; Tzung-Jeng Hwang; Christer Halldin; Lars Farde
Journal:  J Cereb Blood Flow Metab       Date:  2011-12-14       Impact factor: 6.200

2.  Dose-dependent binding of AZD3783 to brain 5-HT1B receptors in non-human primates and human subjects: a positron emission tomography study with [11C]AZ10419369.

Authors:  Katarina Varnäs; Svante Nyberg; Per Karlsson; M Edward Pierson; Matts Kågedal; Zsolt Cselényi; Dennis McCarthy; Alan Xiao; Minli Zhang; Christer Halldin; Lars Farde
Journal:  Psychopharmacology (Berl)       Date:  2011-01-15       Impact factor: 4.530

3.  Cerebral serotonin release correlates with [11C]AZ10419369 PET measures of 5-HT1B receptor binding in the pig brain.

Authors:  Louise M Jørgensen; Pia Weikop; Claus Svarer; Ling Feng; Sune H Keller; Gitte M Knudsen
Journal:  J Cereb Blood Flow Metab       Date:  2017-07-07       Impact factor: 6.200

4.  Assessing the sensitivity of [¹¹C]p943, a novel 5-HT1B radioligand, to endogenous serotonin release.

Authors:  Kelly P Cosgrove; Tracy Kloczynski; Nabeel Nabulsi; David Weinzimmer; Shu-Fei Lin; Julie K Staley; Zubin Bhagwagar; Richard E Carson
Journal:  Synapse       Date:  2011-05-03       Impact factor: 2.562

5.  Synthesis and evaluation of two new candidate high-affinity full agonist PET radioligands for imaging 5-HT1B receptors.

Authors:  Anton Lindberg; Shuiyu Lu; Sangram Nag; Magnus Schou; Jeih-San Liow; Sami S Zoghbi; Michael P Frankland; Robert L Gladding; Cheryl L Morse; Akihiro Takano; Nahid Amini; Charles S Elmore; Yong Sok Lee; Robert B Innis; Christer Halldin; Victor W Pike
Journal:  Nucl Med Biol       Date:  2019-01-26       Impact factor: 2.408

6.  Test-retest reliability of [11C]AZ10419369 binding to 5-HT(1B) receptors in human brain.

Authors:  Magdalena Nord; Sjoerd J Finnema; Martin Schain; Christer Halldin; Lars Farde
Journal:  Eur J Nucl Med Mol Imaging       Date:  2013-09-05       Impact factor: 9.236

7.  Serotonin transporter occupancy by escitalopram and citalopram in the non-human primate brain: a [(11)C]MADAM PET study.

Authors:  Sjoerd J Finnema; Christer Halldin; Benny Bang-Andersen; Christoffer Bundgaard; Lars Farde
Journal:  Psychopharmacology (Berl)       Date:  2015-05-17       Impact factor: 4.530

8.  The effect of early trauma exposure on serotonin type 1B receptor expression revealed by reduced selective radioligand binding.

Authors:  James W Murrough; Christoph Czermak; Shannan Henry; Nabeel Nabulsi; Jean-Dominique Gallezot; Ralitza Gueorguieva; Beata Planeta-Wilson; John H Krystal; John F Neumaier; Yiyun Huang; Yu-Shin Ding; Richard E Carson; Alexander Neumeister
Journal:  Arch Gen Psychiatry       Date:  2011-09

9.  Sensitivity of [(11)C]ORM-13070 to increased extracellular noradrenaline in the CNS - a PET study in human subjects.

Authors:  Jussi Lehto; Jarkko Johansson; Lauri Vuorilehto; Pauliina Luoto; Eveliina Arponen; Harry Scheinin; Juha Rouru; Mika Scheinin
Journal:  Psychopharmacology (Berl)       Date:  2015-04-29       Impact factor: 4.530

Review 10.  Identifying serotonergic mechanisms underlying the corticolimbic response to threat in humans.

Authors:  Patrick M Fisher; Ahmad R Hariri
Journal:  Philos Trans R Soc Lond B Biol Sci       Date:  2013-02-25       Impact factor: 6.237
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