Structure-activity relationship for A series of 2-substituted 1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indoles : Potent subtype-selective inhibitors of N-methyl-D-aspartate (NMDA) receptors

A series of 2-substituted 1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indoles was synthesized as potential antagonists for the NR1A/2B subtype of N-methyl-D-aspartate (NMDA) receptors. Assayed by electrical recording under steady-state conditions, 7-hydroxy-2-(4-phenylbutyl)- 1,2,3,4-tetrahydropyrido-[3,4-b]...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1999-06, Vol.9 (11), p.1619-1624
Hauptverfasser:	TAMIZ, A. P, WHITTEMORE, E. R, WOODWARD, R. M, UPASANI, R. B, KEANA, J. F. W
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Glutamatergic system (aspartate and other excitatory aminoacids) Indoles - chemical synthesis Indoles - chemistry Indoles - pharmacology Inhibitory Concentration 50 Medical sciences Models, Chemical Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Pyridines - chemical synthesis Pyridines - pharmacology Receptors, N-Methyl-D-Aspartate - antagonists & inhibitors Structure-Activity Relationship Xenopus - embryology
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Zusammenfassung:	A series of 2-substituted 1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indoles was synthesized as potential antagonists for the NR1A/2B subtype of N-methyl-D-aspartate (NMDA) receptors. Assayed by electrical recording under steady-state conditions, 7-hydroxy-2-(4-phenylbutyl)- 1,2,3,4-tetrahydropyrido-[3,4-b]indole (30) was the most potent compound in the series having an IC50 value of 50 nM at the NR1A/2B receptors.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(99)00248-6