569351-25-3Relevant academic research and scientific papers
Compound as potassium channel modulator
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Paragraph 0706; 0749; 0751; 0758; 0759, (2018/07/30)
The invention relates to a compound as a potassium channel modulator, which is a compound of a formula (I) or a pharmaceutically acceptable salt thereof. The compound or the pharmaceutically acceptable salt thereof is effective for curing and preventing diseases and symptoms influenced by the activity of potassium ion channels.
Binding of tetrahydrocarboline derivatives at human 5-HT5A receptors
Khorana, Nantaka,Smith, Carol,Herrick-Davis, Kathy,Purohit, Anil,Teitler, Milt,Grella, Brian,Dukat, Ma?gorzata,Glennon, Richard A.
, p. 3930 - 3937 (2007/10/03)
On the basis of an earlier finding that 5-methyl-5H-1,2,3,4-tetrahydropyrido[4,3-b]indole (5-methyl-1,2,3,4-tetrahydro-γ-carboline; 1) binds at murine 5-HT 5A receptors, preliminary structure-affinity studies were conducted. The present investigation extends these structure-affinity studies using human 5-HT5A receptors and examined additional analogues of 1. It was found (a) that there is little interspecies difference for the affinities of these compounds, (b) that an intact 1,2,3,4-tetrahydro-γ-carboline ring system seems optimal and an N2-(3-(substituted-phenoxy)propyl) moiety results in high affinity, (c) that structurally related 1,2,3,4-tetrahydro-β-carbolines also bind at 5-HT5A receptors, and (d) that all examined derivatives also possess affinity for 5-HT 2A receptors. Evidence is provided that 5-HT5A and 5-HT2A receptor affinities probably do not covary and that it might be possible, with continued investigation, to develop analogues with enhanced 5-HT5A selectivity.
