Discovery of 3-Substituted Aminocyclopentanes as Potent and Orally Bioavailable NR2B Subtype-Selective NMDA Antagonists

A series of 3-substituted aminocyclopentanes has been identified as highly potent and selective NR2B receptor antagonists. Incorporation of a 1,2,4-oxadiazole linker and substitution of the pendant phenyl ring led to the discovery of orally bioavailable analogues that showed efficient NR2B receptor...

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Veröffentlicht in:	ACS chemical neuroscience 2011-07, Vol.2 (7), p.352-362
Hauptverfasser:	Layton, Mark E., Kelly, Michael J., Rodzinak, Kevin J., Sanderson, Philip E., Young, Steven D., Bednar, Rodney A., DiLella, Anthony G., Mcdonald, Terrence P., Wang, Hao, Mosser, Scott D., Fay, John F., Cunningham, Michael E., Reiss, Duane R., Fandozzi, Christine, Trainor, Nicole, Liang, Annie, Lis, Edward V., Seabrook, Guy R., Urban, Mark O., Yergey, James, Koblan, Kenneth S.
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Animals Benzopyrans - metabolism Biological Availability Catalepsy - chemically induced Catalepsy - drug therapy Cyclopentanes - chemical synthesis Cyclopentanes - pharmacology Dogs Drug Discovery - methods ERG1 Potassium Channel Ether-A-Go-Go Potassium Channels - antagonists & inhibitors Ether-A-Go-Go Potassium Channels - metabolism Excitatory Amino Acid Antagonists - chemical synthesis Excitatory Amino Acid Antagonists - pharmacology Female Half-Life Indicators and Reagents Isomerism Ligation Macaca mulatta Male Neuralgia - drug therapy Oxadiazoles - chemical synthesis Oxadiazoles - pharmacology Parkinson Disease - drug therapy Piperidines - metabolism Pyrimidines - chemical synthesis Pyrimidines - pharmacology Rats Rats, Sprague-Dawley Receptors, N-Methyl-D-Aspartate - antagonists & inhibitors Spinal Nerves - pathology
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