In an attempt to further improve the a-adrenoreceptor blocking activity of benextramine, the effect of heteroaromaticsubstituents on the terminal nitrogens was studied. In this communication we report on the newly synthetizedN,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-fo1d) than benextramine. These preliminary results show thatpyrextramine can replace benextramine in the elucidation and characlerizatron of the peripheral ar-adrenoreceptors.
N,N"-(DITHIO-2,1-ETIIANEDIYL)BIS{N'-(PYRROL-2-YLMETI{YL)-1,6-HEXANEDIAMINE}(PYREXTRAMINE), A NEW IRREVERSIBLE a,.ADRENORECEPTOR BLOCKING AGENTTHE TETRAMINE DISULFIDE CLASS / Brasili, Livio; EGLE BRANCIA, PIERO A. N. G. E. L. I.; Carlo, Melchiorre. - In: EUROPEAN JOURNAL OF PHARMACOLOGY. - ISSN 0014-2999. - STAMPA. - 103:(1984), pp. 181-184.
N,N"-(DITHIO-2,1-ETIIANEDIYL)BIS{N'-(PYRROL-2-YLMETI{YL)-1,6-HEXANEDIAMINE}(PYREXTRAMINE), A NEW IRREVERSIBLE a,.ADRENORECEPTOR BLOCKING AGENTTHE TETRAMINE DISULFIDE CLASS
BRASILI, Livio;
1984
Abstract
In an attempt to further improve the a-adrenoreceptor blocking activity of benextramine, the effect of heteroaromaticsubstituents on the terminal nitrogens was studied. In this communication we report on the newly synthetizedN,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-fo1d) than benextramine. These preliminary results show thatpyrextramine can replace benextramine in the elucidation and characlerizatron of the peripheral ar-adrenoreceptors.
Pubblicazioni consigliate
I metadati presenti in IRIS UNIMORE sono rilasciati con licenza Creative Commons CC0 1.0 Universal, mentre i file delle pubblicazioni sono rilasciati con licenza Attribuzione 4.0 Internazionale (CC BY 4.0), salvo diversa indicazione.
In caso di violazione di copyright, contattare Supporto Iris
