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New pyrimido[5,4-b]indoles and [1]benzothieno[3,2-d]pyrimidines: high affinity ligands for the alpha(1)-adrenoceptor subtypes |
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| Authors: | Romeo Giuseppe Materia Luisa Marucci Gabriella Modica Maria Pittalà Valeria Salerno Loredana Siracusa Maria Angela Buccioni Michela Angeli Piero Minneman Kenneth P |
| Institution: | Dipartimento di Scienze Farmaceutiche, Università di Catania, viale A. Doria 6, 95125 Catania, Italy. gromeo@unict.it |
| Abstract: | A number of new pyrimido5,4-b]indole and 1]benzothieno3,2-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. |
| Keywords: | α 1-Adrenoceptor Ligand Antagonist Synthesis α 1D-Adrenoceptor subtype |
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