5(10-]9)ABEO-ERGOLINE DERIVATIVES - SYNTHESIS, 5-HT1A-RECEPTOR AFFINITY AND SELECTIVITY

The synthesis and the structure-affinity relationship (S.A.F.I.R.) stu dy for the 5-HT1A receptor sites of a novel series of 5(10-->9)abeo-er goline derivatives are presented. Most derivatives showed moderate to high affinity and selectivity for 5-HT1A receptor sites. The structure -affinity relationship pointed out the role of the substituent at posi tion 8, and the outstanding importance of the reduction of the indole 2,3-double bond for achieving the highest 5-HT1A affinity and selectiv ity within the compounds presented. (C) Elsevier, Paris.