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...

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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
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cited_by cdi_FETCH-LOGICAL-c248t-994c86be946e0104daca0f1d8a1041c9596ae0e23c3f7bd39b419ca3d2a6d4b3
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container_issue 9
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container_title Bioorganic & medicinal chemistry letters
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creator BÖHME, Thomas M
KEIM, Christine
DANNHARDT, Gerd
MUTSCHLER, Ernst
LAMBRECHT, Günter
description 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.
doi_str_mv 10.1016/S0960-894X(01)00186-X
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ispartof Bioorganic & medicinal chemistry letters, 2001-05, Vol.11 (9), p.1241-1243
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1464-3405
language eng
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source Elsevier
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
title Design and pharmacology of quinuclidine derivatives as M2-selective muscarinic receptor ligands
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