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[(11)C]MK-4232: The First Positron Emission Tomography Tracer for the Calcitonin Gene-Related Peptide Receptor.
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-Bohórquez, 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.
Afiliação
  • Bell IM; 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.
  • Gallicchio SN; 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.
  • Stump CA; 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.
  • Bruno JG; 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.
  • Fan H; 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.
  • Gantert LT; 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.
  • Hostetler ED; 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.
  • Kemmerer AL; 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.
  • McWherter M; 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.
  • Moore EL; 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.
  • Mosser SD; 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.
  • Purcell ML; 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.
  • Riffel K; 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.
  • Salvatore CA; 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.
  • Sanabria-Bohórquez S; 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.
  • Staas DD; 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.
  • White RB; 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.
  • Williams M; 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.
  • Zartman CB; 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.
  • Cook JJ; 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.
  • Hargreaves RJ; 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.
  • Kane SA; 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.
  • Graham SL; 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.
  • Selnick HG; 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.
ACS Med Chem Lett ; 4(9): 863-8, 2013 Sep 12.
Article em En | MEDLINE | ID: mdl-24900761
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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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Revista: ACS Med Chem Lett Ano de publicação: 2013 Tipo de documento: Article País de afiliação: Estados Unidos

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Revista: ACS Med Chem Lett Ano de publicação: 2013 Tipo de documento: Article País de afiliação: Estados Unidos