N,N''-(dithio-2,1-ethanediyl)bis[N'-(pyrrol-2-ylmethyl)-1, 6,- hexanediamine] (pyrextramine), a new irreversible alpha 1-adrenoreceptor blocking agent of the tetramine disulfide class.
In an attempt to further improve the alpha-adrenoreceptor blocking activity of benextramine, the effect of heteroaromatic substituents on the terminal nitrogens was studied. In this communication we report on the newly synthetized N,N''-(dithio-2,1-ethanediyl)bis[N'-(pyrrol-2-ylmethyl)-1,6- hexanediamine] (pyrextramine) that displayed higher affinity (5-10-fold) and higher selectivity (about 12-fold) than benextramine. These preliminary results show that pyrextramine can replace benextramine in the elucidation and characterization of the peripheral alpha 1-adrenoreceptors.
D000317:Adrenergic alpha-Antagonists / Q000494:pharmacology*; D000818:Animals; D003538:Cystamine / Q000031:analogs & derivatives* / Q000494:pharmacology; D066298:In Vitro Techniques; D007583:Jejunum / Q000378:metabolism; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D051381:Rats; D011919:Rats, Inbred Strains; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects; D011976:Receptors, Muscarinic / Q000187:drug effects; D014649:Vas Deferens / Q000378:metabolism
D000317:Adrenergic alpha-Antagonists; D011942:Receptors, Adrenergic, alpha; D011976:Receptors, Muscarinic; C029998:benextramine; C043084:pyrextramine; D003538:Cystamine