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Updated: Apr 28, 2026

Detection and Quantification of Calcitonin Gene-Related Peptide CGRP in Human Plasma Using a Modified Enzyme-Linked Immunosorbent Assay
Published on: June 16, 2023
[(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
1Departments 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.
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