Design and pharmacology of quinuclidine derivatives as M2-selective muscarinic receptor ligands

In our search for M2-selective muscarinic receptor antagonists, we synthesized 1,3-disubstituted indenes. The effects of different basic moieties with regard to binding and selectivity towards the five distinct muscarinic receptor subtypes were investigated. The results show that the quinuclidine se...

Full description

Saved in:
Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2001-05, Vol.11 (9), p.1241-1243
Main Authors: BÖHME, Thomas M, KEIM, Christine, DANNHARDT, Gerd, MUTSCHLER, Ernst, LAMBRECHT, Günter
Format: Article
Language:English
Subjects:
Alzheimer Disease - diagnostic imaging
Biological and medical sciences
Cholinergic system
Humans
In Vitro Techniques
Ligands
Medical sciences
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pharmacology. Drug treatments
Quinuclidines - chemical synthesis
Quinuclidines - pharmacology
Radiopharmaceuticals - chemical synthesis
Receptor, Muscarinic M2
Receptors, Muscarinic - drug effects
Tomography, Emission-Computed
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:In our search for M2-selective muscarinic receptor antagonists, we synthesized 1,3-disubstituted indenes. The effects of different basic moieties with regard to binding and selectivity towards the five distinct muscarinic receptor subtypes were investigated. The results show that the quinuclidine series afforded the most promising compounds in terms of both receptor affinity and M2-subtype selectivity.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(01)00186-X