Literature DB >> 9342787

PET-characterization of [carbonyl-11C]WAY-100635 binding to 5-HT1A receptors in the primate brain.

L Farde1, N Ginovart, H Ito, C Lundkvist, V W Pike, J A McCarron, C Halldin.   

Abstract

[carbonyl-11C]WAY-100635 is a new radioligand which can be used with positron emission tomography (PET) to provide high contrast delineation of human brain regions that are rich in 5-HT1A receptors. In the present PET study, the binding of [carbonyl-11C]WAY-100635 was characterized in the cynomolgus monkey brain. Pretreatment with each of the two reference compounds, WAY-100635 and 8-OH-DPAT, as well as the drugs buspirone and pindolo, induced a marked inhibition of [carbonyl-11C]WAY-100635 binding in the neocortex and the raphe nuclei. A preliminary Scatchard analysis yielded 5-HT1A receptor density values of the same order as those that have been reported in vitro. The study shows that [carbonyl-11C]WAY-100635 binds specifically to 5-HT1A receptors in the primate brain and has potential for determination of 5-HT1A receptor occupancy and density in psychiatric patients.

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Year:  1997        PMID： 9342787     DOI： 10.1007/s002130050391

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


  16 in total

1.  Measurement of 5-HT(1A) receptor density and in-vivo binding parameters of [(18)F]mefway in the nonhuman primate.

Authors:  Dustin W Wooten; Ansel T Hillmer; Jeffrey M Moirano; Elizabeth O Ahlers; Maxim Slesarev; Todd E Barnhart; Jogeshwar Mukherjee; Mary L Schneider; Bradley T Christian
Journal:  J Cereb Blood Flow Metab       Date:  2012-04-04       Impact factor: 6.200

2.  Clozapine binds preferentially to cortical D1-like dopamine receptors in the primate brain: a PET study.

Authors:  Yuan-Hwa Chou; Christer Halldin; Lars Farde
Journal:  Psychopharmacology (Berl)       Date:  2006-01-05       Impact factor: 4.530

Review 3.  Considerations in the Development of Reversibly Binding PET Radioligands for Brain Imaging.

Authors:  Victor W Pike
Journal:  Curr Med Chem       Date:  2016       Impact factor: 4.530

4.  An in vivo comparison of cis- and trans-[18F]mefway in the nonhuman primate.

Authors:  Dustin Wooten; Ansel Hillmer; Dhanabalan Murali; Todd Barnhart; Mary L Schneider; Jogeshwar Mukherjee; Bradley T Christian
Journal:  Nucl Med Biol       Date:  2011-07-07       Impact factor: 2.408

5.  Occupancy of dopamine D₂ and D₃ and serotonin 5-HT₁A receptors by the novel antipsychotic drug candidate, cariprazine (RGH-188), in monkey brain measured using positron emission tomography.

Authors:  Nicholas Seneca; Sjoerd J Finnema; István Laszlovszky; Béla Kiss; Attila Horváth; Gabriella Pásztor; Margó Kapás; István Gyertyán; Sándor Farkas; Robert B Innis; Christer Halldin; Balázs Gulyás
Journal:  Psychopharmacology (Berl)       Date:  2011-05-28       Impact factor: 4.530

6.  Increase in serotonin-1A autoreceptors in the midbrain of suicide victims with major depression-postmortem evidence for decreased serotonin activity.

Authors:  C A Stockmeier; L A Shapiro; G E Dilley; T N Kolli; L Friedman; G Rajkowska
Journal:  J Neurosci       Date:  1998-09-15       Impact factor: 6.167

7.  Serotonin 1A receptor availability in patients with schizophrenia and schizo-affective disorder: a positron emission tomography imaging study with [11C]WAY 100635.

Authors:  W Gordon Frankle; Ilise Lombardo; Lawrence S Kegeles; Mark Slifstein; John H Martin; Yiyun Huang; Dah-Ren Hwang; Elisa Reich; Claudine Cangiano; Roberto Gil; Marc Laruelle; Anissa Abi-Dargham
Journal:  Psychopharmacology (Berl)       Date:  2006-09-05       Impact factor: 4.530

8.  Synthesis and initial evaluation of [11C](R)-RWAY in monkey-a new, simply labeled antagonist radioligand for imaging brain 5-HT1A receptors with PET.

Authors:  Julie A McCarron; Sami S Zoghbi; H Umesha Shetty; Eric S Vermeulen; Håkan V Wikström; Masanori Ichise; Fumihiko Yasuno; Christer Halldin; Robert B Innis; Victor W Pike
Journal:  Eur J Nucl Med Mol Imaging       Date:  2007-06-20       Impact factor: 9.236

9.  Synthesis and Evaluation of Pyridyloxypyridyl Indole Carboxamides as Potential PET Imaging Agents for 5-HT2C Receptors.

Authors:  Fanxing Zeng; Jonathon A Nye; Ronald J Voll; Leonard Howell; Mark M Goodman
Journal:  ACS Med Chem Lett       Date:  2018-02-05       Impact factor: 4.345

Review 10.  PET radiotracers: crossing the blood-brain barrier and surviving metabolism.

Authors:  Victor W Pike
Journal:  Trends Pharmacol Sci       Date:  2009-07-16       Impact factor: 14.819
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