title: [(11)C]MK-4232: The First Positron Emission Tomography Tracer for the Calcitonin Gene-Related Peptide Receptor.
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.
authors.affiliation: 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.
authors.forename: Ian M
authors.initials: IM
authors.lastname: Bell
authors.affiliation: 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.
authors.forename: Steven N
authors.initials: SN
authors.lastname: Gallicchio
authors.affiliation: 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.
authors.forename: Craig A
authors.initials: CA
authors.lastname: Stump
authors.affiliation: 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.
authors.forename: Joseph G
authors.initials: JG
authors.lastname: Bruno
authors.affiliation: 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.
authors.forename: Hong
authors.initials: H
authors.lastname: Fan
authors.affiliation: 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.
authors.forename: Liza T
authors.initials: LT
authors.lastname: Gantert
authors.affiliation: 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.
authors.forename: Eric D
authors.initials: ED
authors.lastname: Hostetler
authors.affiliation: 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.
authors.forename: Amanda L
authors.initials: AL
authors.lastname: Kemmerer
authors.affiliation: 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.
authors.forename: Melody
authors.initials: M
authors.lastname: McWherter
authors.affiliation: 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.
authors.forename: Eric L
authors.initials: EL
authors.lastname: Moore
authors.affiliation: 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.
authors.forename: Scott D
authors.initials: SD
authors.lastname: Mosser
authors.affiliation: 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.
authors.forename: Mona L
authors.initials: ML
authors.lastname: Purcell
authors.affiliation: 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.
authors.forename: Kerry
authors.initials: K
authors.lastname: Riffel
authors.affiliation: 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.
authors.forename: Christopher A
authors.initials: CA
authors.lastname: Salvatore
authors.affiliation: 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.
authors.forename: Sandra
authors.initials: S
authors.lastname: Sanabria-Bohórquez
authors.affiliation: 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.
authors.forename: Donnette D
authors.initials: DD
authors.lastname: Staas
authors.affiliation: 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.
authors.forename: Rebecca B
authors.initials: RB
authors.lastname: White
authors.affiliation: 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.
authors.forename: Mangay
authors.initials: M
authors.lastname: Williams
authors.affiliation: 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.
authors.forename: C Blair
authors.initials: CB
authors.lastname: Zartman
authors.affiliation: 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.
authors.forename: Jacquelynn J
authors.initials: JJ
authors.lastname: Cook
authors.affiliation: 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.
authors.forename: Richard J
authors.initials: RJ
authors.lastname: Hargreaves
authors.affiliation: 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.
authors.forename: Stefanie A
authors.initials: SA
authors.lastname: Kane
authors.affiliation: 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.
authors.forename: Samuel L
authors.initials: SL
authors.lastname: Graham
authors.affiliation: 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.
authors.forename: Harold G
authors.initials: HG
authors.lastname: Selnick
keywords: MK-4232; calcitonin gene-related peptide receptor; positron emission tomography