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ACS Med Chem Lett. 2013 Jul 18;4(9):863-8. doi: 10.1021/ml400199p. eCollection 2013 Sep 12.

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

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1
Departments of Medicinal Chemistry, Pain & Migraine, Imaging, In Vitro Pharmacology, Neuroscience & Ophthalmology, and Pharmacokinetics Pharmacodynamics & Drug Metabolism, Merck Research Laboratories , West Point, Pennsylvania 19486, United States.

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.

KEYWORDS:

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

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