Serotonergic ergoline derivatives.
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-HT1A or 5-HT2 affinity and selectivity respectively.
Mantegani
S
S
Pharmacia & Upjohn S.p.A.-CNS Research, Nerviano, Milan, Italy. sergio.mantegani@eu.pnu.com
Brambilla
E
E
Caccia
C
C
Damiani
G
G
Fornaretto
M G
MG
McArthur
R A
RA
Varasi
M
M
D000818:Animals; D001667:Binding, Competitive; D015195:Drug Design; D004873:Ergolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006624:Hippocampus / Q000378:metabolism; D007202:Indicators and Reagents; D017397:Prefrontal Cortex / Q000378:metabolism; D011869:Radioligand Assay; D051381:Rats; D011942:Receptors, Adrenergic, alpha / Q000378:metabolism*; D011954:Receptors, Dopamine / Q000378:metabolism*; D011985:Receptors, Serotonin / Q000378:metabolism*; D044263:Receptors, Serotonin, 5-HT1; D017366:Serotonin Receptor Agonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
D004873:Ergolines; D007202:Indicators and Reagents; D011942:Receptors, Adrenergic, alpha; D011954:Receptors, Dopamine; D011985:Receptors, Serotonin; D044263:Receptors, Serotonin, 5-HT1; D017366:Serotonin Receptor Agonists