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]indole (30) was the most potent compound in the series having an IC50 value of 50 nM at the NR1A/2B receptors.
Tamiz
A P
AP
Department of Chemistry, University of Oregon, Eugene 97403, USA.
Whittemore
E R
ER
Woodward
R M
RM
Upasani
R B
RB
Keana
J F
JF
D000818:Animals; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D011725:Pyridines / Q000138:chemical synthesis / Q000494:pharmacology; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D014981:Xenopus / Q000196:embryology
D007211:Indoles; D011725:Pyridines; D016194:Receptors, N-Methyl-D-Aspartate