Synthesis and characterization of bifunctional ligands for β-adrenergic and dopamine D2 receptors: = Synthese und Charakterisierung bifunktionaler Liganden für β-adrenerge und Dopamin D2 Rezeptoren
Saved in:
| Main Author: | |
|---|---|
| Format: | Thesis Book |
| Language: | English |
| Published: |
Erlangen ; Nürnberg
[2018]
|
| Subjects: | |
| Online Access: | Inhaltsverzeichnis Inhaltsverzeichnis |
| Physical Description: | 280 Seiten Illustrationen, Diagramme 21 cm |
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MARC
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| 100 | 1 | |a Schwalbe, Tobias |d 1988- |e Verfasser |0 (DE-588)1182461255 |4 aut | |
| 245 | 1 | 0 | |a Synthesis and characterization of bifunctional ligands for β-adrenergic and dopamine D2 receptors |b = Synthese und Charakterisierung bifunktionaler Liganden für β-adrenerge und Dopamin D2 Rezeptoren |c vorgelegt von Tobias Schwalbe |
| 246 | 1 | 3 | |a Synthese und Charakterisierung bifunktionaler Liganden für β-adrenerge und Dopamin D2 Rezeptoren |
| 246 | 1 | 1 | |a Synthese und Charakterisierung bifunktionaler Liganden für β-adrenerge und Dopamin D2 Rezeptoren |
| 264 | 1 | |a Erlangen ; Nürnberg |c [2018] | |
| 300 | |a 280 Seiten |b Illustrationen, Diagramme |c 21 cm | ||
| 336 | |b txt |2 rdacontent | ||
| 337 | |b n |2 rdamedia | ||
| 338 | |b nc |2 rdacarrier | ||
| 502 | |b Dissertation |c Friedrich-Alexander-Universität Erlangen-Nürnberg |d 2018 | ||
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| 650 | 0 | 7 | |a Beta-Rezeptor |0 (DE-588)4144967-8 |2 gnd |9 rswk-swf |
| 650 | 0 | 7 | |a Dopaminantagonist |0 (DE-588)4299915-7 |2 gnd |9 rswk-swf |
| 655 | 7 | |0 (DE-588)4113937-9 |a Hochschulschrift |2 gnd-content | |
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| 999 | |a oai:aleph.bib-bvb.de:BVB01-031247646 | ||
Record in the Search Index
| _version_ | 1804180003473063936 |
|---|---|
| adam_text | TABLE
OF
CONTENTS
1.
INTRODUCTION
.................................................................................................................................
1
1.1.
G
PROTEIN
COUPLED
RECEPTORS
.................................................................................................
2
1.1.1.
P-ADRENERGIC
RECEPTORS
..........................................................................................................
2
1.1.2.
DOPAMINERGIC
RECEPTORS
........................................................................................................
4
1.1.3.
RHODOPSIN
-
A
PROTOTYPE
OF
A
NATURAL
COVALENT
LIGAND-RECEPTOR
COMPLEX
...........................
4
1.2.
COVALENTLY
BINDING
PROBES
FOR
G
PROTEIN
COUPLED
RECEPTORS
...............................................
5
1.2.1.
THE
SCOPE
OF
COVALENTLY BINDING
PROBES
FOR
GPCRS
..............................................................
6
1.2.2.
CHEMOREACTIVE
PROBES
FOR
ADRENERGIC
AND
DOPAMINERGIC
RECEPTORS
..................................
6
2.
OBJECTIVES
OF
THE
THESIS
................................................................................................................
10
3.
DEVELOPMENT
OF
A
COVALENTLY
BINDING
PARTIAL
AGONIST
FOR
THE
P
2
AR
.........................................
13
3.1.
RATIONAL
DESIGN
.....................................................................................................................
13
3.2.
SYNTHESIS
...............................................................................................................................
15
3.3.
RADIOLIGAND
BINDING
STUDIES
................................................................................................24
3.4.
RADIOLIGAND
DEPLETION
EXPERIMENTS
...................................................................................
25
3.5.
FUNCTIONAL
CHARACTERIZATION
.................................................................................................
26
4.
DESIGN
AND
SYNTHESIS
OF
COVALENTLY
BINDING
P-AR
ANTAGONISTS
................................................
29
4.1. RATIONAL
DESIGN
....................................................................................................................
29
4.2.
SYNTHESIS
...............................................................................................................................
30
4.3. RADIOLIGAND
BINDING
STUDIES
.................................................................................................41
4.4. RADIOLIGAND
DEPLETION
ASSAYS
..............................................................................................
43
5.
IRREVERSIBLY
BINDING
ANTAGONIST
FOR
THE
DOPAMINE
RECEPTOR
D
2
R
BASED
ON
HALOPERIDOL
.......47
5.1.
RATIONAL
DESIGN
....................................................................................................................
47
5.2.
SYNTHESIS
...............................................................................................................................48
5.3.
RADIOLIGAND
BINDING
STUDIES
.................................................................................................
54
5.4.
RADIOLIGAND
DEPLETION
EXPERIMENTS
...................................................................................
56
5.5.
COMPUTATIONAL
DOCKING
.......................................................................................................
58
6.
SYNTHESIS
OF
POTENTIALLY
BIAS
INDUCING
SALMETEROL
DERIVATIVES
FOR
THE
P
2
AR
...........................60
6.1.
RATIONAL
DESIGN
....................................................................................................................
60
6.2.
SYNTHESIS
...............................................................................................................................
60
6.3.
RADIOLIGAND
BINDING
STUDIES
.................................................................................................
63
6.4.
FUNCTIONAL
CHARACTERIZATION
.................................................................................................
64
7.
SYNTHESIS
OF
NORADRENALINE
ANALOGS
FOR
THE
DEVELOPMENT
OF
DNA
NANOSWITCHES
................
67
7.1.
RATIONAL
DESIGN
....................................................................................................................
67
7.2.
SYNTHESIS
..............................................................................................................................
68
7.3.
RADIOLIGAND
BINDING
STUDIES
................................................................................................
70
8.
INVESTIGATIONS
ON
THE
REACTIVITY
OF
DERIVATIVES
OF
THE
P-AR
ANTAGONIST
(S)-PROPRANOLOL
BEARING
VARIOUS
CHEMOREACTIVE
BINDING
GROUPS................................................................................
71
8.1.
RATIONAL
DESIGN
....................................................................................................................
71
8.2.
SYNTHESIS
..............................................................................................................................
73
8.3.
RADIOLIGAND
BINDING
STUDIES
.................................................................................................
77
8.4.
RADIOLIGAND
DEPLETION
EXPERIMENTS
.....................................................................................
79
9.
REVERSIBLE
AND
IRREVERSIBLE
P-AR
LIGANDS
TO
PROMOTE
THE
DEVELOPMENT
OF
NOVEL
COVALENT,
FLUORESCENT
LIGANDS
..............................................................................................................................
84
9.1.
RATIONAL
DESIGN
....................................................................................................................84
9.2.
SYNTHESIS
..............................................................................................................................
87
9.3.
RADIOLIGAND
BINDING
STUDIES
................................................................................................
91
9.4.
RADIOLIGAND
DEPLETION
EXPERIMENTS
...................................................................................
93
10.
SUMMARY
......................................................................................................................................97
11.
ZUSAMMENFASSUNG
....................................................................................................................
106
12.
EXPERIMENTAL
SECTION................................................................................................................
116
12.1.
MATERIAL
AND
METHODS
......................................................................................................
116
12.2.
CHEMICAL
REACTIVITY
STUDIES
...............................................................................................
119
12.3.
EXPERIMENTAL
PROCEDURES
AND
COMPOUND
CHARACTERIZATION
...........................................
121
13.
REFERENCES
..................................................................................................................................
260
14.
APPENDIX
....................................................................................................................................273
15.
CURRICULUM
VITAE
..................................................................................................................280
|
| any_adam_object | 1 |
| author | Schwalbe, Tobias 1988- |
| author_GND | (DE-588)1182461255 |
| author_facet | Schwalbe, Tobias 1988- |
| author_role | aut |
| author_sort | Schwalbe, Tobias 1988- |
| author_variant | t s ts |
| building | Verbundindex |
| bvnumber | BV045864223 |
| ctrlnum | (OCoLC)1113833074 (DE-599)DNB1182460232 |
| discipline | Chemie / Pharmazie Medizin |
| format | Thesis Book |
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| id | DE-604.BV045864223 |
| illustrated | Illustrated |
| indexdate | 2024-07-10T08:28:51Z |
| institution | BVB |
| language | English |
| oai_aleph_id | oai:aleph.bib-bvb.de:BVB01-031247646 |
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| owner_facet | DE-29T DE-29 DE-355 DE-BY-UBR |
| physical | 280 Seiten Illustrationen, Diagramme 21 cm |
| publishDate | 2018 |
| publishDateSearch | 2018 |
| publishDateSort | 2018 |
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| spelling | Schwalbe, Tobias 1988- Verfasser (DE-588)1182461255 aut Synthesis and characterization of bifunctional ligands for β-adrenergic and dopamine D2 receptors = Synthese und Charakterisierung bifunktionaler Liganden für β-adrenerge und Dopamin D2 Rezeptoren vorgelegt von Tobias Schwalbe Synthese und Charakterisierung bifunktionaler Liganden für β-adrenerge und Dopamin D2 Rezeptoren Erlangen ; Nürnberg [2018] 280 Seiten Illustrationen, Diagramme 21 cm txt rdacontent n rdamedia nc rdacarrier Dissertation Friedrich-Alexander-Universität Erlangen-Nürnberg 2018 Agonist (DE-588)4380725-2 gnd rswk-swf Bifunktionelle Verbindungen (DE-588)4298742-8 gnd rswk-swf Beta-Rezeptor (DE-588)4144967-8 gnd rswk-swf Dopaminantagonist (DE-588)4299915-7 gnd rswk-swf (DE-588)4113937-9 Hochschulschrift gnd-content Dopaminantagonist (DE-588)4299915-7 s Beta-Rezeptor (DE-588)4144967-8 s Agonist (DE-588)4380725-2 s Bifunktionelle Verbindungen (DE-588)4298742-8 s DE-604 B:DE-101 application/pdf http://d-nb.info/1182460232/04 Inhaltsverzeichnis DNB Datenaustausch application/pdf http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=031247646&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA Inhaltsverzeichnis |
| spellingShingle | Schwalbe, Tobias 1988- Synthesis and characterization of bifunctional ligands for β-adrenergic and dopamine D2 receptors = Synthese und Charakterisierung bifunktionaler Liganden für β-adrenerge und Dopamin D2 Rezeptoren Agonist (DE-588)4380725-2 gnd Bifunktionelle Verbindungen (DE-588)4298742-8 gnd Beta-Rezeptor (DE-588)4144967-8 gnd Dopaminantagonist (DE-588)4299915-7 gnd |
| subject_GND | (DE-588)4380725-2 (DE-588)4298742-8 (DE-588)4144967-8 (DE-588)4299915-7 (DE-588)4113937-9 |
| title | Synthesis and characterization of bifunctional ligands for β-adrenergic and dopamine D2 receptors = Synthese und Charakterisierung bifunktionaler Liganden für β-adrenerge und Dopamin D2 Rezeptoren |
| title_alt | Synthese und Charakterisierung bifunktionaler Liganden für β-adrenerge und Dopamin D2 Rezeptoren |
| title_auth | Synthesis and characterization of bifunctional ligands for β-adrenergic and dopamine D2 receptors = Synthese und Charakterisierung bifunktionaler Liganden für β-adrenerge und Dopamin D2 Rezeptoren |
| title_exact_search | Synthesis and characterization of bifunctional ligands for β-adrenergic and dopamine D2 receptors = Synthese und Charakterisierung bifunktionaler Liganden für β-adrenerge und Dopamin D2 Rezeptoren |
| title_full | Synthesis and characterization of bifunctional ligands for β-adrenergic and dopamine D2 receptors = Synthese und Charakterisierung bifunktionaler Liganden für β-adrenerge und Dopamin D2 Rezeptoren vorgelegt von Tobias Schwalbe |
| title_fullStr | Synthesis and characterization of bifunctional ligands for β-adrenergic and dopamine D2 receptors = Synthese und Charakterisierung bifunktionaler Liganden für β-adrenerge und Dopamin D2 Rezeptoren vorgelegt von Tobias Schwalbe |
| title_full_unstemmed | Synthesis and characterization of bifunctional ligands for β-adrenergic and dopamine D2 receptors = Synthese und Charakterisierung bifunktionaler Liganden für β-adrenerge und Dopamin D2 Rezeptoren vorgelegt von Tobias Schwalbe |
| title_short | Synthesis and characterization of bifunctional ligands for β-adrenergic and dopamine D2 receptors |
| title_sort | synthesis and characterization of bifunctional ligands for β adrenergic and dopamine d2 receptors synthese und charakterisierung bifunktionaler liganden fur β adrenerge und dopamin d2 rezeptoren |
| title_sub | = Synthese und Charakterisierung bifunktionaler Liganden für β-adrenerge und Dopamin D2 Rezeptoren |
| topic | Agonist (DE-588)4380725-2 gnd Bifunktionelle Verbindungen (DE-588)4298742-8 gnd Beta-Rezeptor (DE-588)4144967-8 gnd Dopaminantagonist (DE-588)4299915-7 gnd |
| topic_facet | Agonist Bifunktionelle Verbindungen Beta-Rezeptor Dopaminantagonist Hochschulschrift |
| url | http://d-nb.info/1182460232/04 http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=031247646&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA |
| work_keys_str_mv | AT schwalbetobias synthesisandcharacterizationofbifunctionalligandsforbadrenergicanddopamined2receptorssyntheseundcharakterisierungbifunktionalerligandenfurbadrenergeunddopamind2rezeptoren AT schwalbetobias syntheseundcharakterisierungbifunktionalerligandenfurbadrenergeunddopamind2rezeptoren |
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