title: New pyrimido[5,4-b]indoles and [1]benzothieno[3,2-d]pyrimidines: high affinity ligands for the alpha(1)-adrenoceptor subtypes.
abstract: 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.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Catania, viale A. Doria 6, 95125 Catania, Italy. gromeo@unict.it
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Romeo
authors.forename: Luisa
authors.initials: L
authors.lastname: Materia
authors.forename: Gabriella
authors.initials: G
authors.lastname: Marucci
authors.forename: Maria
authors.initials: M
authors.lastname: Modica
authors.forename: Valeria
authors.initials: V
authors.lastname: Pittalà
authors.forename: Loredana
authors.initials: L
authors.lastname: Salerno
authors.forename: Maria Angela
authors.initials: MA
authors.lastname: Siracusa
authors.forename: Michela
authors.initials: M
authors.lastname: Buccioni
authors.forename: Piero
authors.initials: P
authors.lastname: Angeli
authors.forename: Kenneth P
authors.initials: KP
authors.lastname: Minneman
mesh_terms: 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
chemical_list: D007211:Indoles; D008024:Ligands; D011743:Pyrimidines; D018340:Receptors, Adrenergic, alpha-1