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.
1984
103
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; 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.
Brasili, Livio; EGLE BRANCIA, PIERO A. N. G. E. L. I.; Carlo, Melchiorre
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11380/743372
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