1,3-Dioxolane-based compounds (2−14) were synthesized, and the pharmacological profiles at α1-adrenoceptor subtypes were assessed by functional experiments in isolated rat vas deferens (α1A), spleen (α1B), and aorta (α1D). Compound 9, with a pA2 of 7.53, 7.36, and 8.65 at α1A, α1B, and α1D, respectively, is the most potent antagonist of the series, while compound 10 with a pA2 of 8.37 at α1D subtype and selectivity ratios of 162 (α1D/α1A) and 324 (α1D/α1B) is the most selective. Binding assays in CHO cell membranes expressing human cloned α1-adrenoceptor subtypes confirm the pharmacological profiles derived from functional experiments, although the selectivity values are somewhat lower. Therefore, it is concluded that 1,3-dioxolane-based ligands are a new class of α1-adrenoceptor antagonists.
1,3-Dioxolane-Based Ligands as a Novel Class of Alpha1-Adrenoceptor Antagonists / Brasili, Livio; Sorbi, Claudia; Franchini, Silvia; Manicardi, M.; Angeli, P.; Marucci, G.; Leonardi, A.; Poggesi, E.. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 46:8(2003), pp. 1504-1511. [10.1021/jm021078o]
Data di pubblicazione: | 2003 | |
Titolo: | 1,3-Dioxolane-Based Ligands as a Novel Class of Alpha1-Adrenoceptor Antagonists | |
Autore/i: | Brasili, Livio; Sorbi, Claudia; Franchini, Silvia; Manicardi, M.; Angeli, P.; Marucci, G.; Leonardi, A.; Poggesi, E. | |
Autore/i UNIMORE: | ||
Digital Object Identifier (DOI): | http://dx.doi.org/10.1021/jm021078o | |
Rivista: | ||
Volume: | 46 | |
Fascicolo: | 8 | |
Pagina iniziale: | 1504 | |
Pagina finale: | 1511 | |
Codice identificativo ISI: | WOS:000182036100026 | |
Codice identificativo Scopus: | 2-s2.0-0037431380 | |
Codice identificativo Pubmed: | 12672251 | |
Citazione: | 1,3-Dioxolane-Based Ligands as a Novel Class of Alpha1-Adrenoceptor Antagonists / Brasili, Livio; Sorbi, Claudia; Franchini, Silvia; Manicardi, M.; Angeli, P.; Marucci, G.; Leonardi, A.; Poggesi, E.. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 46:8(2003), pp. 1504-1511. [10.1021/jm021078o] | |
Tipologia | Articolo su rivista |
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