96649-40-0Relevant academic research and scientific papers
Structure-Activity Relationships for Prazosin and WB 4101 Analogues as α1-Adrenoreceptor Antagonists
Giardina, Dario,Bertini, Rosaria,Brancia, Egle,Brasili, Livio,Melchiorre, Carlo
, p. 1354 - 1357 (2007/10/02)
Several α-adrenoreceptor antagonists were prepared by coupling one of the two moieties of WB 4101 (1) with one of the two moieties of prazosin (2).Their blocking activity and relative selectivity on α1- and α2-adrenoreceptors were evaluated in the isolated rat vas deferens.Although retaining a significant selectivity toward α1-adrenoreceptors, all the drugs were weaker antagonists than the parent compounds 1 and 2.Opening the piperazine ring of 2 gave 3, which displayed a very high activity and selectivity toward α1-adrenoreceptors (α1/α2 = 3890).This may have relevance in understanding the mode of action of prazosin.In addition, 3 may represent a valuable tool in the characterization of α-adrenoreceptor subtypes.
