Literature DB >> 24900761

[(11)C]MK-4232: The First Positron Emission Tomography Tracer for the Calcitonin Gene-Related Peptide Receptor.

Ian M Bell1, Steven N Gallicchio1, Craig A Stump1, Joseph G Bruno1, Hong Fan1, Liza T Gantert1, Eric D Hostetler1, Amanda L Kemmerer1, Melody McWherter1, Eric L Moore1, Scott D Mosser1, Mona L Purcell1, Kerry Riffel1, Christopher A Salvatore1, Sandra Sanabria-Bohórquez1, Donnette D Staas1, Rebecca B White1, Mangay Williams1, C Blair Zartman1, Jacquelynn J Cook1, Richard J Hargreaves1, Stefanie A Kane1, Samuel L Graham1, Harold G Selnick1.   

Abstract

Rational modification of the potent calcitonin gene-related peptide (CGRP) receptor antagonist MK-3207 led to a series of analogues with enhanced CNS penetrance and a convenient chemical handle for introduction of a radiolabel. A number of (11)C-tracers were synthesized and evaluated in vivo, leading to the identification of [(11)C]8 ([(11)C]MK-4232), the first positron emission tomography tracer for the CGRP receptor.

Entities:  

Keywords:  MK-4232; calcitonin gene-related peptide receptor; positron emission tomography

Year:  2013        PMID： 24900761      PMCID： PMC4027146          DOI： 10.1021/ml400199p

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  16 in total

1.  MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.

Authors:  Ian M Bell; Craig A Stump; Steven N Gallicchio; Donnette D Staas; C Blair Zartman; Eric L Moore; Nova Sain; Mark Urban; Joseph G Bruno; Amy Calamari; Amanda L Kemmerer; Scott D Mosser; Christine Fandozzi; Rebecca B White; Matthew M Zrada; Harold G Selnick; Samuel L Graham; Joseph P Vacca; Stefanie A Kane; Christopher A Salvatore
Journal:  Bioorg Med Chem Lett       Date:  2012-04-30       Impact factor: 2.823

2.  BI 44370 TA, an oral CGRP antagonist for the treatment of acute migraine attacks: results from a phase II study.

Authors:  Hans-Christoph Diener; Piero Barbanti; Carl Dahlöf; Uwe Reuter; Julia Habeck; Jana Podhorna
Journal:  Cephalalgia       Date:  2010-12-20       Impact factor: 6.292

Review 3.  The global burden of headache: a documentation of headache prevalence and disability worldwide.

Authors:  Lj Stovner; K Hagen; R Jensen; Z Katsarava; Rb Lipton; Ai Scher; Tj Steiner; J-A Zwart
Journal:  Cephalalgia       Date:  2007-03       Impact factor: 6.292

Review 4.  CGRP and its receptors provide new insights into migraine pathophysiology.

Authors:  Tony W Ho; Lars Edvinsson; Peter J Goadsby
Journal:  Nat Rev Neurol       Date:  2010-09-07       Impact factor: 42.937

5.  Potent, orally bioavailable calcitonin gene-related peptide receptor antagonists for the treatment of migraine: discovery of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1- (2,2,2-trifluoroethyl)azepan-3-yl]-4- (2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin- 1-yl)piperidine-1-carboxamide (MK-0974).

Authors:  Daniel V Paone; Anthony W Shaw; Diem N Nguyen; Christopher S Burgey; James Z Deng; Stefanie A Kane; Kenneth S Koblan; Christopher A Salvatore; Scott D Mosser; Victor K Johnston; Bradley K Wong; Cynthia M Miller-Stein; James C Hershey; Samuel L Graham; Joseph P Vacca; Theresa M Williams
Journal:  J Med Chem       Date:  2007-10-11       Impact factor: 7.446

6.  Calcitonin gene-related peptide receptor antagonist BIBN 4096 BS for the acute treatment of migraine.

Authors:  Jes Olesen; Hans-Christoph Diener; Ingo W Husstedt; Peter J Goadsby; David Hall; Ulrich Meier; Stephane Pollentier; Lynna M Lesko
Journal:  N Engl J Med       Date:  2004-03-11       Impact factor: 91.245

7.  Efficacy and tolerability of MK-0974 (telcagepant), a new oral antagonist of calcitonin gene-related peptide receptor, compared with zolmitriptan for acute migraine: a randomised, placebo-controlled, parallel-treatment trial.

Authors:  Tony W Ho; Michel D Ferrari; David W Dodick; Vince Galet; James Kost; Xiaoyin Fan; Heather Leibensperger; Samar Froman; Christopher Assaid; Christopher Lines; Hille Koppen; Paul K Winner
Journal:  Lancet       Date:  2008-11-25       Impact factor: 79.321

8.  Pharmacological properties of MK-3207, a potent and orally active calcitonin gene-related peptide receptor antagonist.

Authors:  Christopher A Salvatore; Eric L Moore; Amy Calamari; Jacquelynn J Cook; Maria S Michener; Stacey O'Malley; Patricia J Miller; Cyrille Sur; David L Williams; Zhizhen Zeng; Andrew Danziger; Joseph J Lynch; Christopher P Regan; John F Fay; Yui S Tang; Chi-Chung Li; Nicole T Pudvah; Rebecca B White; Ian M Bell; Steven N Gallicchio; Samuel L Graham; Harold G Selnick; Joseph P Vacca; Stefanie A Kane
Journal:  J Pharmacol Exp Ther       Date:  2010-01-11       Impact factor: 4.030

9.  The discovery of highly potent CGRP receptor antagonists.

Authors:  Craig A Stump; Ian M Bell; Rodney A Bednar; Joseph G Bruno; John F Fay; Steven N Gallicchio; Victor K Johnston; Eric L Moore; Scott D Mosser; Amy G Quigley; Christopher A Salvatore; Cory R Theberge; C Blair Zartman; Xu-Fang Zhang; Stefanie A Kane; Samuel L Graham; Joseph P Vacca; Theresa M Williams
Journal:  Bioorg Med Chem Lett       Date:  2008-10-31       Impact factor: 2.823

Review 10.  CSF as a surrogate for assessing CNS exposure: an industrial perspective.

Authors:  Jiunn H Lin
Journal:  Curr Drug Metab       Date:  2008-01       Impact factor: 3.731
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  2 in total

Review 1.  Recent neuroimaging advances in the study of primary headaches.

Authors:  Amy R Tso; Peter J Goadsby
Journal:  Curr Pain Headache Rep       Date:  2015-06

2.  Calcitonin gene-related peptide (CGRP)-induced recovery after myocardial infarction: Is there a role for CGRP-targeted molecular image-guided strategies in cardiology?

Authors:  Rudolf A Werner; Takahiro Higuchi
Journal:  J Nucl Cardiol       Date:  2021-06-04       Impact factor: 3.872
  2 in total

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