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- W1967142439 abstract "Berberine, an alkaloid, has been found to have a myriad of pharmacological effects including hypotensive, antisecretory, sedative, and antimicrobial effects, some of which are similar to those of clonidine, an α2 adrenoceptor partial agonist. The interaction of berberine with human platelet α2 adrenoceptor was investigated in this study. Berberine was found to inhibit competitively the specific binding of [3H]-yohimbine. The displacement curve was parallel to those of clonidine, epinephrine, norepinephrine, with the rank order of potency (IC50) being clonidine (0.4 μM) > epinephrine (7.5 μM) > norepinephrine (14.5 μM) = berberine (16.6 μM). Increasing concentrations of berberine from 0.1 μM to 10 μM inhibited [3H]-yohimbine binding, shifting the saturation binding curve to the right without decreasing the maximum binding capacity. In platelet cyclic AMP accumulation experiments, berberine at concentrations of 0.1 μM to 0.1 mM inhibited the cAMP accumulation induced by 10 μM prostaglandin E1 in a dose dependent manner, acting as an α2 adrenoceptor agonist. In the presence of L-epinephrine, berberine blocked the inhibitory effect of L-epinephrine behaving as an α2 adrenoceptor antagonist. These properties are similar to those of clonidine of human platelets, suggesting that berberine is a partial agonist of platelet α2 adrenoceptors. These findings may provide potential mechanisms for the hypotensive, antisecretory, and sedative effects of berberine." @default.
- W1967142439 created "2016-06-24" @default.
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- W1967142439 date "1991-01-01" @default.
- W1967142439 modified "2023-09-26" @default.
- W1967142439 title "Interaction of berberine with human platelet α2 adrenoceptors" @default.
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- W1967142439 doi "https://doi.org/10.1016/0024-3205(91)90019-8" @default.
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