| Autor: |
Paolo Pevarello, Philippe Dostert, F Vaghi, Alberto Bonsignori, A Della Torre, Massimo Cini, M. Varasi, M. Meroni, Piero Melloni |
| Rok vydání: |
1991 |
| Předmět: |
|
| Zdroj: |
European Journal of Medicinal Chemistry. 26:207-213 |
| ISSN: |
0223-5234 |
| DOI: |
10.1016/0223-5234(91)90031-h |
| Popis: |
In the search for new antidepressants with a rapid onset of action, fenmetazole analogues, bearing a second phenyl ring in a position previously shown not to be detrimental to affinity and selectivity for the α2-adrenoreceptors, were synthesized in an attempt to combine NA-uptake inhibition and blockade of the α2-adrenoreceptors in the same molecule. Some of the new molecules showed enhanced affinity and selectivity for the α2-adrenoreceptors compared to fenmetazole. Surprisingly, introduction of a phenyl ring in the structure of fenmetazole changed the agonistic action of the parent compound toward the α1-adrenoreceptors into an antagonistic effect. However, none of the new derivatives showed in vitro NA-uptake inhibitory potency substantially different from the low activity of fenmetazole in this test. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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