Modified ibogaine fragments: Synthesis and preliminary pharmacological characterization of 3-ethyl-5-phenyl-1, 2, 3, 4, 5, 6-hexahydroazepino [4, 5-b] …

…, DC Mash, AB Khare, Q Ouyang

文献索引：Efange, Simon M. N.; Mash, Deborah C.; Khare, Anil B.; Ouyang, Quinjie Journal of Medicinal Chemistry, 1998 , vol. 41, # 23 p. 4486 - 4491

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被引用次数: 30

摘要

Five phenyl-substituted derivatives and analogues of 1, 2, 3, 4, 5, 6-hexahydroazepino [4, 5- b] indole, 5, a major fragment of ibogaine (1), were synthesized and tested for binding to monoamine transporters, the NMDA receptor-coupled cation channel, and dopamine and opioid receptors. All five derivatives, 9 and 17a-d, displayed 8-10-fold higher affinity at the DA transporter than ibogaine and noribogaine (4). At the serotonin transporter, two ...