Influence of chain length and N-alkylation on the selective serotonin receptor ligand 9-(aminomethyl)-9, 10-dihydroanthracene

…, JE Savage, M Taroua, BL Roth, RA Glennon…

Index: Runyon, Scott P.; Savage, Jason E.; Taroua, Mohamed; Roth, Bryan L.; Glennon, Richard A.; Westkaemper, Richard B. Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 5 p. 655 - 658

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Citation Number: 16

Abstract

Comparison of the serotonin 5-HT2A receptor affinities of chain lengthened and N-alkylated analogues of the novel ligand 9-aminomethyl-9, 10-dihydroanthracene (AMDA) and a structurally similar prototypical tricyclic amine imipramine suggests that the two agents bind to the receptor in different fashions. The demonstration that AMDA is highly selective for serotonin receptors (5-HT2A, Ki= 20nM; 5-HT2C, Ki= 43nM) versus the dopamine D2 ...