Diphenyl sulfoxides as selective antagonists of the muscarinic M2 receptor

Autor:	Guowei Zhou, Ruth A. Duffy, Herbert Binch, Jean E. Lachowicz, Lisa A. Taylor, William Billard, Derek B. Lowe, Joseph A. Kozlowski, Robert D. McQuade, Gordon Crosby, Vilma Ruperto, Henry Guzik
Rok vydání:	2000
Předmět:	Pyridines Stereochemistry Clinical Biochemistry Administration Oral Pharmaceutical Science Muscarinic Antagonists Naphthalenes Biochemistry Chemical synthesis Structure-Activity Relationship chemistry.chemical_compound Alkaloids Piperidines Dibenzazepines Drug Discovery Muscarinic acetylcholine receptor Benzene Derivatives medicine Animals Humans Structure–activity relationship Furans Receptor Molecular Biology Receptor Muscarinic M2 Organic Chemistry Antagonist Muscarinic antagonist Muscarinic acetylcholine receptor M2 Sulfoxide Receptors Muscarinic Acetylcholine Corpus Striatum Recombinant Proteins Rats chemistry Drug Design Molecular Medicine medicine.drug
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 10:2255-2257
ISSN:	0960-894X
DOI:	10.1016/s0960-894x(00)00438-8
Popis:	Structure activity studies on [4-(phenylsulfonyl)phenyl]methylpiperazine led to the discovery of 4-cyclohexyl-alpha-[4-[[4-methoxyphenyl(S)-sufinyl]phenyl]-1-pi perazineacetonitrile, 1, an M2 selective muscarinic antagonist. Affinity at the cloned human M2 receptor was 2.7 nM; the M1/M2 selectivity is 40-fold.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4687a6dfde6b8966420c582c2ce3bbeb https://doi.org/10.1016/s0960-894x(00)00438-8 Zobrazit plný text záznamu Full Text from ScienceDirect