Structural modifications of arylpiperazine and arylsulfonamide serotonin 5-HT1A and 5-HT7 receptor ligands in search of factors determining selectivity - Digital Medical Library

Skip to main menu
Skip to search engine
Skip to content
Skip to footer

Download

Description
Information

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

Author:

Date:

Type:

Praca doktorska

Abstract:

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.

Place of publishing:

Level of degree:

2 - studia doktoranckie

Degree discipline:

Degree grantor:

Wydział Farmaceutyczny

Promoter:

Bojarski, Andrzej J.

Date issued:

Identifier:

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

Call number:

Language:

Access rights:

Subject and keywords:

5-HT7 5-HT1A receptors serotonin ligands

Object collections:

Digital Medical Library > PhD thesis database

Last modified:

Jun 26, 2023

In our library since:

Nov 21, 2012

Number of object content hits:

1 167

Number of object content views in PDF format

354

All available object's versions:

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

Show description in RDF format:

Show description in OAI-PMH format:

Edition name	Date
ZB-111670	Jun 26, 2023

Objects

Similar

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

Bugno, Ryszard

2010

Praca doktorska

Allosteric modulation of serotonin 5-HT1A and 5 HT7 receptors by zinc ions

Satała, Grzegorz

2017

Praca doktorska

Novel aryl-alkyl-piperazines with N-acylated amino acids as serotoninergic receptors ligands

Zajdel, Paweł

2006

Praca doktorska

Novel anilide and benzylamide derivatives as 5-HT1A/5- HT7 receptor ligands and phosphodiesterase type 4 and 7 inhibitors with potential procognitive and antidepressant activity

Jankowska, Agnieszka Wioleta

2021

Praca doktorska

Chemical and pharmacological studies in group of 3,3-disubstituted derivatives of pyrrolidyne-2,5-dion with potential anticonvulsant activity

Chlebek, Iwona

2013

Praca doktorska

Novel functionally selective agonists of the serotonin 5 HT1A receptor

Śniecikowska, Joanna

2018

Praca doktorska

Spirohydantion - new ligands of central serotonergic system

Czopek, Anna

2008

Praca doktorska

Characteristics of functional selectivity new 5-HT1A serotonin receptor agonists

Głuch-Lutwin, Monika

2022

Praca doktorska

More

Citation style:

Contact details

Address

Medical Library
Medyczna 7
30-688 Krakow

Phone

12 658 72 56
517 385 669

E-Mail

Collecting and Elaboration Department
cyfrowabm@cm-uj.krakow.pl

Visit us!

https://bm.cm.uj.edu.pl/en/main-page/

This page uses 'cookies'. More information