Synthesis and characterization of molecular probes for studying aminergic G-protein coupled receptors:
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| Format: | Thesis Book |
| Language: | English |
| Published: |
2014
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| Subjects: | |
| Online Access: | Inhaltsverzeichnis |
| Physical Description: | 199 S. Ill., graph. Darst. |
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| adam_text | SYNTHESIS AND CHARACTERIZATION OF MOLECULAR
PROBES FOR STUDYING AMINERGIC G PROTEIN-COUPLED
RECEPTORS
DER NATURWISSENSCHAFTLICHEN FAKULTAT
DER FRIEDRICH-ALEXANDER-UNIVERSITAT ERLANGEN-NURNBERG
ZUR
ERLANGUNG DES DOKTORGRADES DR. RER. NAT.
VORGELEGT VON
DIETMAR WIELAND WEICHERT
AUS COBURG
HTTP://D-NB.INFO/1068782919
TABLE OF CONTENTS
1. INTRODUCTION 1
1.1. G PROTEIN-COUPLED RECEPTORS 1
1.1.1. MOLECULAR PROBES FOR GPCRS 3
1.1.2. PROBING STRUCTURE AND
FUNCTION OF GPCRS 5
2. OBJECTIVES OF THE THESIS 10
3. COVALENT
NEUROTRANSMITTER SURROGATES FOR AMINERGIC GPCRS 13
3.1. A GENERAL SYNTHESIS
TO ACCESS COVALENT LIGANDS FOR AMINERGIC GPCRS 15
3.2. BIOLOGICAL
CHARACTERIZATION OF THE COVALENT NEUROTRANSMITTER SURROGATES 21
3.3. STRUCTURAL
STUDIES ON THE P
2
AR
H93C
:
THE PROOF OF CONCEPT 27
3.4. CONCLUSION 32
4. PROBING MOLECULAR DETERMINANTS
FOR BIASED AGONISM AT THE P
2
AR
..33
4.1. DESIGN AND SYNTHESIS OF THE P
2
AR LIGANDS 36
4.1.1. SYNTHESIS OF LIGANDS FEATURING THE AMINO ALCOHOL MOTIF 37
4.1.2. SYNTHESIS OF THE LIGANDS DEVOID OF THE P-HYDROXYL GROUP 44
4.2. FUNCTIONAL CHARACTERIZATION
OF THE FCAR LIGANDS. 47
4.2.1.8-HYDROXYQUINOLIN-2(1H)-ONE-DERIVED LIGANDS 47
4.2.2. 5-HYDROXY-2H-BENZO[B][1,4]OXAZIN-3(4H)-ONE-DERIVED LIGANDS 50
4.3. DISCUSSION AND
CONCLUSION 51
5. SYNTHESIS
AND CHARACTERIZATION
OF NOVEL DOPAMINERGIC AGONISTS
...54
5.1. DESIGN AND SYNTHESIS OF DOPAMINERGIC LIGANDS 57
5.2. BIOLOGICAL
CHARACTERIZATION AT DRS 62
5.2.1. RADIOLIGAND BINDING STUDIES 62
5.2.2. FUNCTIONAL CHARACTERIZATION AT THE D
2
R 64
5.3. DISCUSSION AND CONCLUSION 68
6. FLUORESCENT LIGANDS
FOR THE FEAR 71
6.1. DESIGN AND SYNTHESIS 73
6.2. INITIAL
CHARACTERIZATION OF THE
PRECURSOR 78
7. SUMMARY 79
8. ZUSAMMENFASSUNG 86
9. EXPERIMENTAL SECTION 95
9.1. BIOLOGICAL EXPERIMENTS 95
9.2. CHEMISTRY 98
10. REFERENCES 184
11. LIST
OF ABBREVIATIONS 195
12. CURRICULUM VITAE 199
|
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| dewey-ones | 540 - Chemistry and allied sciences 610 - Medicine and health |
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| dewey-tens | 540 - Chemistry and allied sciences 610 - Medicine and health |
| discipline | Chemie / Pharmazie Medizin |
| format | Thesis Book |
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| indexdate | 2024-07-10T01:20:09Z |
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| language | English |
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| spelling | Weichert, Dietmar Wieland 1983- Verfasser (DE-588)1067872930 aut Synthesis and characterization of molecular probes for studying aminergic G-protein coupled receptors vorgelegt von Dietmar Wieland Weichert 2014 199 S. Ill., graph. Darst. txt rdacontent n rdamedia nc rdacarrier Erlangen-Nürnberg, Univ., Diss., 2014 Ligand Biochemie (DE-588)4606532-5 gnd rswk-swf G-Protein gekoppelter Rezeptor (DE-588)7723480-7 gnd rswk-swf Aminerge Nervenzelle (DE-588)4599577-1 gnd rswk-swf (DE-588)4113937-9 Hochschulschrift gnd-content G-Protein gekoppelter Rezeptor (DE-588)7723480-7 s Aminerge Nervenzelle (DE-588)4599577-1 s Ligand Biochemie (DE-588)4606532-5 s DE-604 DNB Datenaustausch application/pdf http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=027822004&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA Inhaltsverzeichnis |
| spellingShingle | Weichert, Dietmar Wieland 1983- Synthesis and characterization of molecular probes for studying aminergic G-protein coupled receptors Ligand Biochemie (DE-588)4606532-5 gnd G-Protein gekoppelter Rezeptor (DE-588)7723480-7 gnd Aminerge Nervenzelle (DE-588)4599577-1 gnd |
| subject_GND | (DE-588)4606532-5 (DE-588)7723480-7 (DE-588)4599577-1 (DE-588)4113937-9 |
| title | Synthesis and characterization of molecular probes for studying aminergic G-protein coupled receptors |
| title_auth | Synthesis and characterization of molecular probes for studying aminergic G-protein coupled receptors |
| title_exact_search | Synthesis and characterization of molecular probes for studying aminergic G-protein coupled receptors |
| title_full | Synthesis and characterization of molecular probes for studying aminergic G-protein coupled receptors vorgelegt von Dietmar Wieland Weichert |
| title_fullStr | Synthesis and characterization of molecular probes for studying aminergic G-protein coupled receptors vorgelegt von Dietmar Wieland Weichert |
| title_full_unstemmed | Synthesis and characterization of molecular probes for studying aminergic G-protein coupled receptors vorgelegt von Dietmar Wieland Weichert |
| title_short | Synthesis and characterization of molecular probes for studying aminergic G-protein coupled receptors |
| title_sort | synthesis and characterization of molecular probes for studying aminergic g protein coupled receptors |
| topic | Ligand Biochemie (DE-588)4606532-5 gnd G-Protein gekoppelter Rezeptor (DE-588)7723480-7 gnd Aminerge Nervenzelle (DE-588)4599577-1 gnd |
| topic_facet | Ligand Biochemie G-Protein gekoppelter Rezeptor Aminerge Nervenzelle Hochschulschrift |
| url | http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=027822004&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA |
| work_keys_str_mv | AT weichertdietmarwieland synthesisandcharacterizationofmolecularprobesforstudyingaminergicgproteincoupledreceptors |