Abstract
A series of 3-alkylamino-4-(2-((5-dimethylaminomethyl-2-furyl)methylthio)ethylamino)furazans were prepared and tested for their H2-antagonist activities on guinea pig right atrium. A number of differently shaped alkyl substituents on the terminal 3-amino group were favourable for activity. The most potent compound was the cyclohexyl-methyl-substituted derivative (pA2=8.83). Most compounds showed non-competitive antagonism at histamine H1 and muscarinic receptors at concentrations approximately 100 times higher than those producing competitive H2-receptor block. This finding suggests that there is an accessorial binding area on H2-receptor near the site fitted by the diamino-furazan moiety.
Lingua originale | Inglese |
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pagine (da-a) | 475-478 |
Numero di pagine | 4 |
Rivista | European Journal of Medicinal Chemistry |
Volume | 24 |
Numero di pubblicazione | 5 |
DOI | |
Stato di pubblicazione | Pubblicato - 1989 |
Pubblicato esternamente | Sì |