157767-06-1Relevant academic research and scientific papers
Serotonergic ergoline derivatives
Mantegani, Sergio,Brambilla, Enzo,Caccia, Carla,Damiani, Gabriele,Fornaretto, Maria Gioia,McArthur, Robert A.,Varasi, Mario
, p. 1117 - 1122 (1998)
Novel classes of 13- and 14-tertbutyl-ergoline derivatives were prepared, and characterised in vitro for their affinity for adrenergic, dopaminergic and serotonergic binding sites. This study particularly examines the importance of the presence and the position of the tert-butyl group in conferring either significant 5-HT(1A) or 5-HT2 affinity and selectivity respectively.
Synthesis and in vitro structure-activity relationship of 13-tert- butyl-ergoline derivatives as 5-HT(1A) receptor ligands
Mantegani,Brambilla,Caccia,Fornaretto,Mc Arthur,Varasi
, p. 795 - 804 (1997)
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.
