| Description: |
Tetrahydroberberine, with D(2) receptor antagonist and 5-HT(1A) receptor agonist properties, has significant potential as a therapeutic for treatment of FD; it has antidopaminergic effect, and other pharmacological action on the central nervous system. Tetrahydroberberine can inhibit the rabbit platelet aggregation. |
| Targets: |
5-HT Receptor | Dopamine Receptor |
| In vitro: |
| Acta Crystallogr C Struct Chem. 2015 Apr;71(Pt 4):262-5. | | Tetrahydroberberine, a pharmacologically active naturally occurring alkaloid.[Pubmed: 25836282] |
METHODS AND RESULTS:
Tetrahydroberberine (systematic name: 9,10-dimethoxy-5,8,13,13a-tetrahydro-6H-benzo[g][1,3]benzodioxolo[5,6-a]quinolizine), C20H21NO4, a widely distributed naturally occurring alkaloid, has been crystallized as a racemic mixture about an inversion center. A bent conformation of the molecule is observed, with an angle of 24.72 (5)° between the arene rings at the two ends of the reduced quinolizinium core.
CONCLUSIONS:
The intermolecular hydrogen bonds that play an apparent role in crystal packing are 1,3-benzodioxole -CH2···OCH3 and -OCH3···OCH3 interactions between neighboring molecules. |
|
| In vivo: |
| J Pharmacol Exp Ther. 2011 Sep;338(3):917-24. | | Tetrahydroberberine, an isoquinoline alkaloid isolated from corydalis tuber, enhances gastrointestinal motor function.[Pubmed: 21659472] |
METHODS AND RESULTS:
Oral administration of Tetrahydroberberine not only resulted in significantly accelerated gastric emptying of normal rats in a bell-shaped relationship, with a maximal efficacy at a dose of 30 μg/kg, but also restored the delayed gastric emptying caused by apomorphine, which might be mediated by an antidopaminergic effect. Data from electromyography indicated enhanced motor function of the upper gastrointestinal tract by Tetrahydroberberine , which occurred through strengthening contractility and shortening the contraction interval. Oral administration of Tetrahydroberberine resulted in a drastic increase of gastric accommodation in Beagle dogTetrahydroberberine(30 μg/kg, p < 0.01) and comparable with that of sumatriptan (3 mg/kg), a potent fundic relaxant.
CONCLUSIONS:
Taken together, our data suggested that Tetrahydroberberine, with D(2) receptor antagonist and 5-HT(1A) receptor agonist properties, has significant potential as a therapeutic for treatment of FD. |
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