Abstract
The S and R isomers of [18F]-fluoropropranolol (1-[1-fluoro-2-isopropylamino]-3-naphthalen-1-yloxy-propan-2 -ol) have been prepared by reductive alkylation of the appropriate aminoalcohols. The radiosynthesis provides a reasonable yield (approximately 25%) to give products of 99% enantiomeric excess and specific activities of 1-3 Ci/micromol. The dissociation constants for the beta2 adrenergic receptor are 0.5 and 2.5 nM for the S and the R isomers, respectively. The biodistribution data in rats show that uptake and egress of the tracer is rapid but that the result of blocking studies and the difference between the R and the S isomers suggest receptor-mediated uptake in receptor-rich tissue.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Algorithms
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Animals
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Fluorine Radioisotopes
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Indicators and Reagents
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Isotope Labeling
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Ligands
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Lipids / chemistry
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Male
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Propranolol / analogs & derivatives*
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Propranolol / chemical synthesis
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Propranolol / chemistry
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Propranolol / pharmacokinetics
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Radiopharmaceuticals / chemical synthesis*
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Radiopharmaceuticals / chemistry
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Radiopharmaceuticals / pharmacokinetics
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Rats
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Rats, Sprague-Dawley
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Receptors, Adrenergic, beta / chemistry
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Receptors, Adrenergic, beta / drug effects*
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Solubility
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Solvents
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Stereoisomerism
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Tissue Distribution
Substances
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Fluorine Radioisotopes
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Indicators and Reagents
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Ligands
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Lipids
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Radiopharmaceuticals
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Receptors, Adrenergic, beta
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Solvents
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fluoropropranolol
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Propranolol