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Bioorg Med Chem. 1999 Feb;7(2):287-95.

1,2,3,4-tetrahydroisoquinoline derivatives: a new class of 5-HT1A receptor ligands.

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Department of Medicinal Chemistry, Polish Academy of Sciences, Kraków.


Three series of new N-substituted 1,2,3,4-tetrahydroisoquinolines with 2-, 3-, and 4-membered alkyl chains (a, b, and c, respectively) were synthesized, and the effect of some structural modifications on their 5-HT1A receptor affinities and functional properties was discussed. It was found that the volume of the terminal amide substituent was a crucial parameter which determined 5-HT1A receptor affinities of the tested compounds, while the in vivo activity seemed to depend on both the R-volume and the length of a hydrocarbon chain. It was demonstrated that the most active ligands behaved like agonists or partial agonists at postsynaptic 5-HT1A receptors.

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