95688-34-9Relevant 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 (2007/10/03)
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 antihypertensive activity of 2,4-dioxoimidazolidin-1-yl and perhydro-2,4-dioxopyrimidin-1-yl ergoline derivatives
Mantegani, Sergio,Brambilla, Enzo,Caccia, Carla,Chiodini, Laura,Ruggieri, Daniela,Lamberti, Ernesto,Di Salle, Enrico,Salvati, Patricia
, p. 293 - 304 (2007/10/03)
The synthesis and antihypertensive activity of a series of 2,4-dioxoimidazoldin-1-yl and perhydro-2,4-dioxopyrimidin-1-yl ergoline derivatives are reported. The oral antihypertensive activity was studied in spontaneously hypertensive rats (SHRs) by measuring systolic blood pressure by an indirect tail-cuff method at different times after treatment. The prolactin lowering activity (indirectly measured by the nidation test) in rats and the oral acute toxicity in mice were also studied. The results of this study revealed potent antihypertensive ergoline derivatives devoid of side-effects related to the dopaminergic stimulation and the importance of the Δ9,10 double bond for conferring high potency within these compounds.
