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 ( …

…, ER Whittemore, RM Woodward, RB Upasani…

Index: Tamiz, Amir P.; Whittemore, Edward R.; Woodward, Richard M.; Upasani, Ravindra B.; Keana, John F.W. Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 11 p. 1619 - 1624

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Citation Number: 9

Abstract

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.