ABSTRACT The general synthetic methods and α-blocking activity in the rat vas deferens of a series of tetra- and diamine disulfides structurally analogues to benextramine as well as a serie of related compounds without the disulfide group are described. All compounds containing a central cystamine moiety displayed an irreversible α-adrenergic blockade at concentrations ranging from 10-4 to 6 x 10-6 M. Potency was increased in cystamines N, N` -disubstituted with 6-aminohexyl groups, especially when the outer nitrogen atoms bear arylalkyi substituents or are inclosed in a ring.
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