New aza(nor)adamantanes are agonists at the newly identified serotonin 5-HT4 receptor and antagonists at the 5-HT3 receptor

Autor:	Chafiq Moummi, Dai-Chang Yang, Daniel L. Flynn, Roger Nosal, Daniel P. Becker, G. W. Gullikson, Dale P. Spangler
Rok vydání:	1992
Předmět:	biology Stereochemistry Chemistry Organic Chemistry Clinical Biochemistry Pharmaceutical Science 5-HT4 receptor Pharmacology Biochemistry 5-HT3 receptor Drug Discovery biology.protein Molecular Medicine Agonism Serotonin Antagonism Receptor Molecular Biology
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 2:1613-1618
ISSN:	0960-894X
DOI:	10.1016/s0960-894x(00)80441-2
Popis:	New aza(nor)adamantanes 1A , 1B , and 1C are described which exhibit properties of both 5-HT4 agonism and 5-HT3 antagonism. In particular, compound 1C [SC-52491], an azanoradamantane, exhibits an EC50 of 51 nM in a functional model of 5-HT4 agonism and potent antagonism, Ki = 1.2 nM, at the 5-HT3 receptor.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::ee8ca2120c6861af925b4314701bf4e8 https://doi.org/10.1016/s0960-894x(00)80441-2 Zobrazit plný text záznamu