Synthesis, radiofluorination and pharmacological evaluation of a fluoromethyl spirocyclic PET tracer for central σ 1 receptors and comparison with fluoroalkyl homologs

Bioorganic and Medicinal Chemistry

Volumn 20, Issue 1, 2012, Pages 257-269

  Maisonial, Aurélie ^b   Große Maestrup, Eva ^a   Wiese, Christian ^a   Hiller, Achim ^b   Schepmann, Dirk ^a   Fischer, Steffen ^b   Deuther Conrad, Winnie ^b   Steinbach, Jörg ^b   Brust, Peter ^b   Wünsch, Bernhard ^a  

^a UNIVERSITY OF MÜNSTER   (Germany)

^b INSTITUTE OF ION BEAM PHYSICS AND MATERIALS RESEARCH   (Germany)

Author keywords

1 Receptor radioligands; Fluorine 18; Fluoroalkyl homologs; Neuroimaging; Spirocyclic piperidines; Structure affinity relationship

Indexed keywords

1' (4 FLUOROBENZYL) 3 (FLUOROMETHYL) 3H SPIRO([2]BENZOFURAN 1,4' PIPERIDINE); 1' (4 FLUOROBENZYL) 3 METHYL 3H SPIRO([2]BENZOFURAN 1,4' PIPERIDINE); 1' BENZYL 3 (FLUOROMETHYL) 3H SPIRO([2]BENZOFURAN 1,4' PIPERIDINE); 1' BENZYL 3H SPIRO([2]BENZOFURAN 1,4' PIPERIDINE) 3 CARBONITRILE; 3 (FLUOROMETHYL) 1' (1 PHENYLETHYL) 3H SPIRO([2]BENZOFURAN 1,4' PIPERIDINE); 3 (FLUOROMETHYL) 3H SPIRO([2]BENZOFURAN 1,4' PIPERIDINE); 3 METHYL 1' (1 PHENYLETHYL) 3H SPIRO([2]BENZOFURAN 1,4' PIPERIDINE); 3 METHYL 3H SPIRO([2]BENZOFURAN 1,4' PIPERIDINE); 3 METHYL 3H SPIRO([2]BENZOFURAN 1,4' PIPERIDINE) 3 CARBOXYLATE; [1' BENZYL 3H SPIRO([2]BENZOFURAN 1,4' PIPERIDIN) 3 YL]METHANOL; DIMETHYL SULFOXIDE; ETHYL 1' BENZYL 3H SPIRO([2]BENZOFURAN 1,4' PIPERIDINE); FLUORINE 18; PIPERIDINE DERIVATIVE; RADIOPHARMACEUTICAL AGENT; SIGMA 1 OPIATE RECEPTOR; UNCLASSIFIED DRUG;

ANIMAL TISSUE; ARTICLE; BIOTRANSFORMATION; COMPLEX FORMATION; CONTROLLED STUDY; DRUG BRAIN LEVEL; DRUG STABILITY; DRUG SYNTHESIS; DRUG TARGETING; DRUG UPTAKE; FLUORINATION; IN VITRO STUDY; ISOTOPE LABELING; LIPOPHILICITY; METABOLITE; NONHUMAN; POSITRON EMISSION TOMOGRAPHY; RADIATION DOSE DISTRIBUTION; TEMPERATURE SENSITIVITY;

ANIMALS; BRAIN; FLUORINE RADIOISOTOPES; ISOTOPE LABELING; LIGANDS; MICE; MICROSOMES, LIVER; POSITRON-EMISSION TOMOGRAPHY; RADIOPHARMACEUTICALS; RATS; RECEPTORS, SIGMA; SPIRO COMPOUNDS; TISSUE DISTRIBUTION;

MUS;

EID: 84855194939     PISSN: 09680896     EISSN: 14643391     Source Type: Journal    
DOI: 10.1016/j.bmc.2011.11.002     Document Type: Article

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