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Tytuł: Structural modifications of arylpiperazine and arylsulfonamide serotonin 5-HT1A and 5-HT7 receptor ligands in search of factors determining selectivity

Autor:

Bugno, Ryszard

Data:

2010

Typ:

Praca doktorska

Abstrakt:

The PhD thesis focuses on structural factors determining selectivity of arylpiperazine and arylsulfonamide derivatives for 5-HTlA and 5-HT7 receptors. The synthesis and SAR analysis of pyrrolidine and benzotriazole derivatives confirmed that linearly extended conformation of LCAP is bioactive for 5-HTlA receptors, whereas this geometry is unfavorable for the 5-HT7 receptors. In the group of benzisoxazolepiperazine derivatives the use of sulfonamide fragment, additionally rigidified by the piperidine ring, is significant for high affinity for 5-HT7R; however, the activity toward 5-HT1AR (and others monoaminergic receptors) is not completely eliminated. It was found, that the lack of aromatic groups m the vicinity of protonated nitrogen atom (perhydroisoquinoline derivatives) is essential for selectivity to 5-HT7R vs 5-HT1AR. Docking studies showed that these ligands are located between helices 3, 6 and 7, within the so-called selective part of 5-HT7R binding pocket. Moreover, based on new arylsulfonamide derivatives the 3D QSAR pharmacophore model was generated. It extends the previous selectivity hypothesis (obtained in structure-based approach), by defining the additional hydrophobic region, located near aromatic feature.

Miejsce wydania:

Kraków

Stopień studiów:

2 - studia doktoranckie

Dyscyplina:

farmakologia

Instytucja nadająca tytuł:

Wydział Farmaceutyczny

Promotor:

Bojarski, Andrzej J.

Data wydania:

2009

Identyfikator:

oai:dl.cm-uj.krakow.pl:760

Sygnatura:

ZB-111670

Język:

pol

Prawa dostępu:

nieograniczony

Temat i słowa kluczowe:

5-HT7 5-HT1A receptors serotonin ligands

Kolekcje, do których przypisany jest obiekt:

Data ostatniej modyfikacji:

26 cze 2023

Data dodania obiektu:

21 lis 2012

Liczba wyświetleń treści obiektu:

1 116

Liczba wyświetleń treści obiektu w formacie PDF

229

Wszystkie dostępne wersje tego obiektu:

http://dl.cm-uj.krakow.pl:8080/publication/760

Wyświetl opis w formacie RDF:

RDF

Wyświetl opis w formacie OAI-PMH:

OAI-PMH

Nazwa wydania Data
ZB-111670 26 cze 2023

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Adres

Biblioteka Medyczna
ul. Medyczna 7
30-688 Kraków

Telefon

12 658 72 56
517 385 669

E-Mail

Oddział Gromadzenia i Opracowania Zbiorów
cyfrowabm@cm-uj.krakow.pl

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