Development of 18F-labelled radioligands for molecular imaging of the dopamine D4 receptor:
Gespeichert in:
| 1. Verfasser: | |
|---|---|
| Format: | Abschlussarbeit Buch |
| Sprache: | English |
| Veröffentlicht: |
Jülich
Forschungszentrum Jülich
2011
|
| Schriftenreihe: | Schriften des Forschungszentrums Jülich
Reihe Gesundheit ; Bd. 43 |
| Schlagworte: | |
| Online-Zugang: | Inhaltsverzeichnis |
| Beschreibung: | XIV, 161 S. 240 mm x 170 mm |
| ISBN: | 9783893367382 |
Internformat
MARC
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| 245 | 1 | 0 | |a Development of 18F-labelled radioligands for molecular imaging of the dopamine D4 receptor |c Fabian Kügler |
| 264 | 1 | |a Jülich |b Forschungszentrum Jülich |c 2011 | |
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Datensatz im Suchindex
| _version_ | 1804148709767774208 |
|---|---|
| adam_text | IMAGE 1
INDEX
1. INTRODUCTION 1
2. BASICS AND METHODS 3
2.1 IMAGING O F NEUROFUNCTIONS W I T H POSITRON EMISSION T O M O G R A P
H Y (PET) 3
2.2 STEPS O F RADIOLIGAND DEVELOPMENT 5
2.2.1 PRECEDING CONSIDERATIONS 6
2.2.2 SELECTION AND PRODUCTION O F SHORT-LIVED POSITRON EMITTING
RADIONUCLIDES
ESPECIALLY FLUORINE-18 7
2.2.3 DEVELOPMENT O F LABELLING METHODS W I T H FLUORINE-18 9
2.2.4 SPECIAL METHODS IN N.C.A. LSF-FLUORINATION 12
2.2.5 PHARMACOLOGICAL EVALUATION O F RADIOLIGANDS F O R T H E CENTRAL
NERVOUS SYSTEM 19
2.3 DOPAMINE RECEPTORS AND LIGANDS 2 4
2.3.1 SUBTYPES O F DOPAMINE R E C E P T O R S - T H E D 4 R E C E P T O
R 24
2.3.2 DOPAMINE D 4 R E C E P T O R SUBTYPE-SELECTIVE LIGANDS 27
2.4 LIPOPHILICITY - A KEY PROPERTY F O R RADIOLIGANDS 32
3. AIMS AND SCOPE 37
4. SYNTHESIS AND 18 F-LABELLING OF FAUC 316 39
4.1 SYNTHESES O F STANDARD AND PRECURSOR COMPOUNDS 4 0
4.1.1 FORMATION O F 2-CARBOXYLIC INDOLE VIA PALLADIUM MEDIATED
INTRAMOLECULAR
COUPLING 4 1
4.1.2 FORMATION O F 2-CARBOXYLIC INDOLE BY INTRAMOLECULAR REDUCTIVE
AMINATION 4 3
4.1.3 REDUCTION O F 5-CYANO-2-CARBOXYINDOLE ESTER 4 4
4.1.4 SYNTHESES O F IODONIUM PRECURSORS 4 6
4.2 RADIOSYNTHESIS O F [ 1SF]FAUC 316 4 7
4.2.1 SYNTHESIS O F 4-[ 18F]FLUOROBROMOBENZENE AND
4-[LSF]FLUOROIODO-BENZENE 4 7
4.2.2 PIPERIDINE AND 1-METHYLPIPERAZINE AS MODEL COMPOUNDS F O R A
RADIOACTIVE
PALLADIUM-CATALYZED BUCHWALD-HARTWIG CROSS-COUPLING 4 9
4.2.3 DIRECT BUCHWALD-HARTWIG COUPLING W I T H
L-BENZYL-2-(PIPERAZINE-L-YL-METHYL)LH-INDOLE-5-CARBONITRILE 5 2
4.2.4 SYNTHESIS O F [ 1SF]FAUC 316 VIA 4-[LSF]FLUOROPHENYLPIPERAZINE 53
4.2.5 PURIFICATION AND ISOLATION O F [ 1SF]FAUC 316 5 8
4.3 PHARMACOLOGICAL EVALUATION O F [ 18F]FAUC 316 63
4.4 INTERIM SUMMARY 6 4
HTTP://D-NB.INFO/1018003975
IMAGE 2
X
5. SYNTHESIS, 18 F-LABELLING AND PRECLINICAL EVALUATION OF BENZODIOXINE
DERIVATIVES 66
5.1 SYNTHESIS O F BENZODIOXINE STANDARD AND PRECURSOR COMPOUNDS F O R
18F-LABELLING 67 5.2 RECEPTOR BINDING AND INTRINSIC AFFINITIES 7 1
5.3 RADIOSYNTHESIS O F BENZODIOXINE DERIVATIVES 75
5.3.1 DIRECT N.C.A. 18F-LABELLING O F BENZODIOXINE DERIVATIVES 75
5.3.2 BUILD-UP SYNTHESIS O F BENZODIOXINE DERIVATIVES BY REDUCTIVE
AMINATION 77
5.3.3 COMPARISON O F 18F-LABELLING METHODS F O R BENZODIOXINE
DERIVATIVES 8 2
5.4 PHARMACOLOGICAL EVALUATION O F 18F-LABELLED BENZODIOXINE DERIVATIVES
AS D 4 LIGANDS 8 4
5.4.1 LIPOPHILICITY 8 4
5.4.2 AUTORADIOGRAPHY 85
5.4.3 BIODISTRIBUTION AND IN VIVO STABILITY 8 8
5.5 INTERIM SUMMARY 9 2
6. EXPERIMENTAL 95
6.1 MATERIALS, CHROMATOGRAPHIC AND SPECTROMETRIC PROCEDURES 95
6.2 SYNTHESIS O F [ 18F]FAUC 316 9 6
6.2.1 SYNTHESES O F PRECURSOR AND STANDARD COMPOUNDS 9 6
6.2.2 RADIOSYNTHESES 108
6.3 SYNTHESIS O F BENZODIOXINE DERIVATIVES 1 1 1
6.3.1 SYNTHESES O F PRECURSOR-AND STANDARD COMPOUNDS 1 1 1
6.3.2 RADIOSYNTHESES 120
6.3.3 RADIOANALYTICAL METHODS 123
6.4 PHARMACOLOGY 1 3 1
6.4.1 DETERMINATION O F PARTITION COEFFICIENTS 1 3 1
6.4.2 ANIMALS 1 3 1
6.4.3 IN VITRO AUTORADIOGRAPHY O F RAT AND MOUSE BRAIN SLICES 132
6.4.4 EX VIVO BIODISTRIBUTION IN MOUSE MODEL 132
6.4.5 IN VIVO STABILITY O F [ 18F]33E 132
6.4.6 STAINING O F BRAIN SLICES BY CRESYL VIOLET 133
7. SUMMARY AND OUTLOOK 135
8. LITERATURE 1 4 1
|
| any_adam_object | 1 |
| author | Kügler, Fabian 1982- |
| author_GND | (DE-588)1017873410 |
| author_facet | Kügler, Fabian 1982- |
| author_role | aut |
| author_sort | Kügler, Fabian 1982- |
| author_variant | f k fk |
| building | Verbundindex |
| bvnumber | BV039786882 |
| ctrlnum | (OCoLC)775076352 (DE-599)DNB1018003975 |
| dewey-full | 616.858907575 |
| dewey-hundreds | 600 - Technology (Applied sciences) |
| dewey-ones | 616 - Diseases |
| dewey-raw | 616.858907575 |
| dewey-search | 616.858907575 |
| dewey-sort | 3616.858907575 |
| dewey-tens | 610 - Medicine and health |
| discipline | Allgemeine Naturwissenschaft Medizin |
| format | Thesis Book |
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| id | DE-604.BV039786882 |
| illustrated | Not Illustrated |
| indexdate | 2024-07-10T00:11:27Z |
| institution | BVB |
| isbn | 9783893367382 |
| language | English |
| oai_aleph_id | oai:aleph.bib-bvb.de:BVB01-024647619 |
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| owner_facet | DE-12 |
| physical | XIV, 161 S. 240 mm x 170 mm |
| publishDate | 2011 |
| publishDateSearch | 2011 |
| publishDateSort | 2011 |
| publisher | Forschungszentrum Jülich |
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| series | Schriften des Forschungszentrums Jülich |
| series2 | Schriften des Forschungszentrums Jülich : Reihe Gesundheit |
| spelling | Kügler, Fabian 1982- Verfasser (DE-588)1017873410 aut Development of 18F-labelled radioligands for molecular imaging of the dopamine D4 receptor Fabian Kügler Jülich Forschungszentrum Jülich 2011 XIV, 161 S. 240 mm x 170 mm txt rdacontent n rdamedia nc rdacarrier Schriften des Forschungszentrums Jülich : Reihe Gesundheit Bd. 43 Zugl.: Köln, Univ., Diss., 2011 (DE-588)4113937-9 Hochschulschrift gnd-content Schriften des Forschungszentrums Jülich Reihe Gesundheit ; Bd. 43 (DE-604)BV035800060 43 DNB Datenaustausch application/pdf http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=024647619&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA Inhaltsverzeichnis |
| spellingShingle | Kügler, Fabian 1982- Development of 18F-labelled radioligands for molecular imaging of the dopamine D4 receptor Schriften des Forschungszentrums Jülich |
| subject_GND | (DE-588)4113937-9 |
| title | Development of 18F-labelled radioligands for molecular imaging of the dopamine D4 receptor |
| title_auth | Development of 18F-labelled radioligands for molecular imaging of the dopamine D4 receptor |
| title_exact_search | Development of 18F-labelled radioligands for molecular imaging of the dopamine D4 receptor |
| title_full | Development of 18F-labelled radioligands for molecular imaging of the dopamine D4 receptor Fabian Kügler |
| title_fullStr | Development of 18F-labelled radioligands for molecular imaging of the dopamine D4 receptor Fabian Kügler |
| title_full_unstemmed | Development of 18F-labelled radioligands for molecular imaging of the dopamine D4 receptor Fabian Kügler |
| title_short | Development of 18F-labelled radioligands for molecular imaging of the dopamine D4 receptor |
| title_sort | development of 18f labelled radioligands for molecular imaging of the dopamine d4 receptor |
| topic_facet | Hochschulschrift |
| url | http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=024647619&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA |
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