187977-46-4Relevant articles and documents
Synthesis and α1-antagonist activity of new prazosin- and benextramine-related tetraamine disulfides
Giardina,Crucianelli,Gulini,Marucci,Melchiorre,Spampinato
, p. 9 - 20 (2007/10/03)
Tetraamine disulfides 1-10 were designed by combining the structural features of benextramine, an irreversible α1/α2-adrenoceptor antagonist, and prazosin, a selective competitive α1-antagonist. Their biological profile was assessed by functional and binding assays. In rat vas deferens functional experiments, tetraamine disulfides 1-10 displayed a marked selectivity at α1-adrenoceptors. Furthermore, they acted as competitive antagonists at α1-adrenoceptors and weak noncompetitive (irreversible) antagonists at α2-adrenoceptors. In binding assays, performed at α1-adrenoceptors of rat liver (α(1B)) and submaxillary gland (α(1A)), compound 5 showed an 11-fold selectivity for α(1B)-adrenoceptors in contrast to both prazosin and benextramine, which were not selective or selective for the α(1A)-subtype respectively.