Title of article :
1,2,3,4-Tetrahydroisoquinoline Derivatives: A New Class of 5-HT1A Receptor Ligands Original Research Article
Author/Authors :
Maria J. Mokrosz، نويسنده , , Andrzej J. Bojarski، نويسنده , , Beata Duszynska، نويسنده , , Ewa Tatarczy?ska، نويسنده , , Aleksandra K?odzi?ska، نويسنده , , Anna Dere?-Weso?ek، نويسنده , , Sijka Charakchieva-Minol، نويسنده , , Ewa Chojnacka-W?jcik، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 1999
Abstract :
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. ©
Keywords :
tetrahydroisoquinoline derivatives , 5-HT1A ligands , Structure–activity relationship
Journal title :
Bioorganic and Medicinal Chemistry
Journal title :
Bioorganic and Medicinal Chemistry