Literature DB >> 17826688

PET tracers for 5-HT(1A) receptors and uses thereof.

J S Dileep Kumar1, J John Mann.   

Abstract

The serotonin 5-HT(1A) receptor is implicated in the pathophysiology of major neuropsychiatric disorders, including depression, suicidal behavior, panic disorder, epilepsy, bulimia, schizophrenia, Parkinson's disease, and Alzheimer's disease and is, therefore, an important target for drug therapy. 5-HT(1A) receptors are expressed as somatodendritic autoreceptors in serotonin neurons of the raphé nuclei (presynaptic) and as postsynaptic receptors in cortical and subcortical serotonin terminal fields in the brain. Due to the higher concentration and heterogeneous distribution of this receptor, it is an attractive target for quantification in vivo using positron emission tomography (PET) and single photon emission tomography (SPECT). Here, we review the PET radioligands employed for imaging 5-HT(1A) receptors in living brain.

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Year:  2007        PMID: 17826688     DOI: 10.1016/j.drudis.2007.07.008

Source DB:  PubMed          Journal:  Drug Discov Today        ISSN: 1359-6446            Impact factor:   7.851


  19 in total

1.  Evaluation of [(11)C]metergoline as a PET radiotracer for 5HTR in nonhuman primates.

Authors:  Jacob M Hooker; Sung Won Kim; Achim T Reibel; David Alexoff; Youwen Xu; Colleen Shea
Journal:  Bioorg Med Chem       Date:  2010-04-20       Impact factor: 3.641

Review 2.  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

3.  First-in-human evaluation of 18F-mefway, a PET radioligand specific to serotonin-1A receptors.

Authors:  Ansel T Hillmer; Dustin W Wooten; Alisha K Bajwa; Andrew T Higgins; Patrick J Lao; Tobey J Betthauser; Todd E Barnhart; Howard A Rowley; Charles K Stone; Sterling C Johnson; Jogeshwar Mukherjee; Bradley T Christian
Journal:  J Nucl Med       Date:  2014-11-13       Impact factor: 10.057

4.  In vivo kinetics of [F-18]MEFWAY: a comparison with [C-11]WAY100635 and [F-18]MPPF in the nonhuman primate.

Authors:  D W Wooten; J D Moraino; A T Hillmer; J W Engle; O J Dejesus; D Murali; T E Barnhart; R J Nickles; R J Davidson; M L Schneider; J Mukherjee; B T Christian
Journal:  Synapse       Date:  2010-12-08       Impact factor: 2.562

5.  Synthesis and Evaluation of Mefway Analogs as Ligands for Serotonin 5HT1A Receptors.

Authors:  Joanne P Thio; Christopher Liang; Alisha K Bajwa; Dustin W Wooten; Bradley T Christian; Jogeshwar Mukherjee
Journal:  Med Chem Res       Date:  2015-04       Impact factor: 1.965

6.  In vivo serotonin-sensitive binding of [11C]CUMI-101: a serotonin 1A receptor agonist positron emission tomography radiotracer.

Authors:  Matthew S Milak; Alin J Severance; Jaya Prabhakaran; J S Dileep Kumar; Vattoly J Majo; R Todd Ogden; J John Mann; Ramin V Parsey
Journal:  J Cereb Blood Flow Metab       Date:  2010-06-23       Impact factor: 6.200

7.  Autoradiographic evaluation of [3H]CUMI-101, a novel, selective 5-HT1AR ligand in human and baboon brain.

Authors:  J S Dileep Kumar; Ramin V Parsey; Suham A Kassir; Vattoly J Majo; Matthew S Milak; Jaya Prabhakaran; Norman R Simpson; Mark D Underwood; J John Mann; Victoria Arango
Journal:  Brain Res       Date:  2013-02-27       Impact factor: 3.252

8.  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

9.  [18F]F15599, a novel 5-HT1A receptor agonist, as a radioligand for PET neuroimaging.

Authors:  Laëtitia Lemoine; Mathieu Verdurand; Bernard Vacher; Elodie Blanc; Didier Le Bars; Adrian Newman-Tancredi; Luc Zimmer
Journal:  Eur J Nucl Med Mol Imaging       Date:  2009-09-30       Impact factor: 9.236

10.  The relation of developmental changes in brain serotonin transporter (5HTT) and 5HT1A receptor binding to emotional behavior in female rhesus monkeys: effects of social status and 5HTT genotype.

Authors:  M Embree; V Michopoulos; J R Votaw; R J Voll; J Mun; J S Stehouwer; M M Goodman; M E Wilson; M M Sánchez
Journal:  Neuroscience       Date:  2012-10-16       Impact factor: 3.590

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