| Autor: |
Tasso, Bruno, Novelli, Federica, Sparatore, Fabio, Fasoli, Francesca, Gotti, Cecilia |
| Zdroj: |
Journal of Natural Products; 20240101, Issue: Preprints |
| Abstrakt: |
(+)-Laburnamine (1), a rare alkaloid extracted from Laburnum anagyroidesseeds (∼4 mg from 1 kg), was shown to bind with high affinity (Ki, 293 nM) to the α4β2 nicotinic receptor subtype, which is, respectively, 126 and 136 times higher than to the α3β4 (Ki37 μM) and α7 subtypes (Ki40 μM). When its ability to release [3H]-dopamine from striatal slices was tested in a functional assay, compound 1behaved as a partial agonist with an EC50of 5.8 μM and an Emaxthat was 43% that of nicotine. When incubated with nicotine in the same assay, 1prevented a maximal effect from being reached. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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