New pyrimido[5,4-b]indoles and [1]benzothieno[3,2-d]pyrimidines: high affinity ligands for the alpha(1)-adrenoceptor subtypes.
A number of new pyrimido[5,4-b]indole and [1]benzothieno[3,2-d]pyrimidine derivatives were synthesized and evaluated for their binding and functional properties at alpha(1)-adrenergic receptor (alpha(1)-AR) subtypes. They behaved as potent alpha(1)-AR antagonists. In binding experiments, some of them (RC24 and RC23) showed very high affinity for the alpha(1D)-AR subtype.
Romeo
Giuseppe
G
Dipartimento di Scienze Farmaceutiche, Università di Catania, viale A. Doria 6, 95125 Catania, Italy. gromeo@unict.it
Materia
Luisa
L
Marucci
Gabriella
G
Modica
Maria
M
Pittalà
Valeria
V
Salerno
Loredana
L
Siracusa
Maria Angela
MA
Buccioni
Michela
M
Angeli
Piero
P
Minneman
Kenneth P
KP
D000818:Animals; D007211:Indoles / Q000138:chemical synthesis / Q000378:metabolism*; D008024:Ligands; D008297:Male; D011467:Prostate / Q000187:drug effects / Q000502:physiology; D011743:Pyrimidines / Q000138:chemical synthesis / Q000378:metabolism*; D051381:Rats; D018340:Receptors, Adrenergic, alpha-1 / Q000502:physiology*; D013329:Structure-Activity Relationship
D007211:Indoles; D008024:Ligands; D011743:Pyrimidines; D018340:Receptors, Adrenergic, alpha-1