Abstract
New carbon-11 and fluorine-18 labeled N-acetyl-1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives were designed and synthesized as potential positron emission tomography AMPA (2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid) receptor ligands to image brain diseases. The single crystal structure of the most potent compound N-acetyl-1-(4'-chlorophenyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline (5a) is first reported.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Amides / chemical synthesis
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Amides / pharmacology*
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Animals
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Anticonvulsants / chemical synthesis*
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Anticonvulsants / pharmacology
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Anticonvulsants / therapeutic use
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Carbon / chemistry
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Fluorine / chemistry
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Isoquinolines / chemical synthesis
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Isoquinolines / pharmacology*
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Isoquinolines / therapeutic use
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Isotope Labeling
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Ligands
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Mice
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Molecular Structure
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Positron-Emission Tomography
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Receptors, AMPA / antagonists & inhibitors*
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Seizures / drug therapy
Substances
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Amides
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Anticonvulsants
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Isoquinolines
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Ligands
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R-4-(3-hydroxyphenyl)-N,N-7,8-tetramethyl-3,4-dihydroisoquinoline-2(1H)-carboxamide
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Receptors, AMPA
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Fluorine
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Carbon