Fused Thiazoloandrostanes and Their Quaternary Salts, Synthesis and Cooperative Ligand Binding to Muscarinic Acetylcholine Receptor

[img]PDF - Authorized users only
Language: English
117Kb
Title:Fused Thiazoloandrostanes and Their Quaternary Salts, Synthesis and Cooperative Ligand Binding to Muscarinic Acetylcholine Receptor
Creators:
Urbanský, Marek
Proška, Jan
Drašar, Pavel
Journal or Publication Title:
Collection of Czechoslovak Chemical Communications, 64, 9, pp. 1457-1470
Uncontrolled Keywords:Muscarinic receptors, Allosteric ligands, Thiazoles, Steroids, Thiazolium salts, Androstane

Abstract

Steroidal thiazolium salts were prepared and their interaction with [<sup>3</sup>H]<i>N</i>-methylscopolamine ([<sup>3</sup>H]NMS) at M<sub>2</sub> muscarinic receptors using radioligand binding were studied. The results were consistent with a ternary complex theory. The compounds diminished [<sup>3</sup>H]NMS binding with <i>K</i><sub>d</sub> values in the micromolar or submicromolar range. In particular, the presence of bulky benzylic group at the thiazole nitrogen atom caused a substantial increase in affinity of allosteric ligand for receptor. Our results demonstrate that steroidal thiazolium salts could be a new class of potentially useful tools for mapping the muscarinic receptors. <p>

Title:Fused Thiazoloandrostanes and Their Quaternary Salts, Synthesis and Cooperative Ligand Binding to Muscarinic Acetylcholine Receptor
Creators:
Urbanský, Marek
Proška, Jan
Drašar, Pavel
Uncontrolled Keywords:Muscarinic receptors, Allosteric ligands, Thiazoles, Steroids, Thiazolium salts, Androstane
Divisions:Life and Chemical Sciences > Institute of Organic Chemistry and Biochemistry > Collection of Czechoslovak Chemical Communications
Journal or Publication Title:Collection of Czechoslovak Chemical Communications
Volume:64
Number:9
Page Range:pp. 1457-1470
ISSN:0010-0765
E-ISSN:1212-6950
Publisher:Institute of Organic Chemistry and Biochemistry
Related URLs:
URLURL Type
http://dx.doi.org/10.1135/cccc19991457UNSPECIFIED
ID Code:1570
Item Type:Article
Deposited On:06 Feb 2009 17:10
Last Modified:06 Feb 2009 16:10

Citation

Urbanský, Marek; Proška, Jan; Drašar, Pavel (1999) Fused Thiazoloandrostanes and Their Quaternary Salts, Synthesis and Cooperative Ligand Binding to Muscarinic Acetylcholine Receptor. Collection of Czechoslovak Chemical Communications, 64 (9). pp. 1457-1470. ISSN 0010-0765

Repository Staff Only: item control page