[(11)C]MK-4232: The First Positron Emission Tomography Tracer for the Calcitonin Gene-Related Peptide Receptor.
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ABSTRACT:
SUBMITTER: Bell IM
PROVIDER: S-EPMC4027146 | biostudies-literature | 2013 Sep
REPOSITORIES: biostudies-literature
Publications
[(11)C]MK-4232: The First Positron Emission Tomography Tracer for the Calcitonin Gene-Related Peptide Receptor.
Bell Ian M IM Gallicchio Steven N SN Stump Craig A CA Bruno Joseph G JG Fan Hong H Gantert Liza T LT Hostetler Eric D ED Kemmerer Amanda L AL McWherter Melody M Moore Eric L EL Mosser Scott D SD Purcell Mona L ML Riffel Kerry K Salvatore Christopher A CA Sanabria-Bohórquez Sandra S Staas Donnette D DD White Rebecca B RB Williams Mangay M Zartman C Blair CB Cook Jacquelynn J JJ Hargreaves Richard J RJ Kane Stefanie A SA Graham Samuel L SL Selnick Harold G HG
ACS medicinal chemistry letters 20130718 9
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. ...[more]
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