Design and synthesis of piperidinyl piperidine analogues as potent and selective M2 muscarinic receptor antagonists

Identification of a number of highly potent M2 receptor antagonists with >100-fold selectivity against the M1 and M3 receptor subtypes is described. In the rat microdialysis assay, this series of compounds showed pronounced enhancement of brain acetylcholine release after oral administration.

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2000-10, Vol.10 (20), p.2247-2250
Hauptverfasser:	YUGUANG WANG, CHACKALAMANNIL, Samuel, MCQUADE, Robert, LACHOWICZ, Jean E, ZHIYONG HU, CLADER, John W, GREENLEE, William, BILLARD, William, BINCH, Herbert III, CROSBY, Gordon, RUPERTO, Vilma, DUFFY, Ruth A
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetylcholine - metabolism Administration, Oral Animals Biological and medical sciences Brain - drug effects Brain - metabolism Cholinergic system Drug Design Medical sciences Microdialysis Muscarinic Antagonists - chemical synthesis Muscarinic Antagonists - chemistry Muscarinic Antagonists - pharmacology Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Piperidines - chemical synthesis Piperidines - chemistry Piperidines - pharmacology Rats Receptor, Muscarinic M1 Receptor, Muscarinic M2 Receptors, Muscarinic - drug effects Receptors, Muscarinic - physiology Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	Identification of a number of highly potent M2 receptor antagonists with >100-fold selectivity against the M1 and M3 receptor subtypes is described. In the rat microdialysis assay, this series of compounds showed pronounced enhancement of brain acetylcholine release after oral administration.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(00)00457-1