- [11C]MK-4232: The first positron emission tomography tracer for the calcitonin gene-related peptide receptor
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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 11C-
- Bell, Ian M.,Gallicchio, Steven N.,Stump, Craig A.,Bruno, Joseph G.,Fan, Hong,Gantert, Liza T.,Hostetler, Eric D.,Kemmerer, Amanda L.,McWherter, Melody,Moore, Eric L.,Mosser, Scott D.,Purcell, Mona L.,Riffel, Kerry,Salvatore, Christopher A.,Sanabria-Bohorquez, Sandra,Staas, Donnette D.,White, Rebecca B.,Williams, Mangay,Zartman, C. Blair,Cook, Jacquelynn J.,Hargreaves, Richard J.,Kane, Stefanie A.,Graham, Samuel L.,Selnick, Harold G.
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supporting information
p. 863 - 868
(2013/10/01)
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- MONOCYCLIC CGRP RECEPTOR ANTAGONISTS
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The present invention is directed to compounds of the formula (I) : (wherein variables A1, A2, A3, A4, A5, A6, A7, A8, G1, G2, G3, G4, J, Q, Ea, Eb, Ec, R6, R7, RPG and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
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