Synthesis and in vitro structure-activity relationship of 13-tert- butyl-ergoline derivatives as 5-HT(1A) receptor ligands

Article abstract of DOI:10.1016/S0223-5234(99)80065-8

A series of novel 13-tert-butyl-ergoline derivatives was prepared and evaluated for affinity to adrenergic, dopaminergic and serotonergic receptor sites. Selectivity for 5-HT(1A) receptors versus α₁, α₂, D₁, D₂, and 5- HT₂ appears to be influenced by the presence of the tert-butyl moiety at position 13 of the ergoline skeleton. Some compounds within this series display nanomolar 5-HT(1A) affinity and hundred-fold selectivity versus the other receptors considered.