Tetrahydroberberine
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.
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Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to
24 months(2-8C).
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
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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.
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.
Neurosci Lett. 1996 Apr 5;207(3):155-8.
Tetrahydroberberine suppresses dopamine-induced potassium current in acutely dissociated CA1 pyramidal neurons from rat hippocampus.[Pubmed:
8728473]
METHODS AND RESULTS:
Effects of Tetrahydroberberine (THB) on dopamine (DA)-induced response have been investigated in single pyramidal neurons freshly dissociated from CA1 area of the hippocampus using the nystatin perforated patch-clamp, whole-cell recording technique under voltage-clamp configuration. Application of Tetrahydroberberine reversibly suppressed three type responses induced by DA with different degrees of inhibitory ratio. Tetrahydroberberine inhibited the DA-induced outward current in a concentration-dependent manner with an IC50 of 13 microM. The maximal value of the concentration-response curve for DA-induced outward current was suppressed by Tetrahydroberberine, suggesting a non-competitive inhibition.
CONCLUSIONS:
The results support the hypothesis that Tetrahydroberberine acts as a novel dopaminergic system antagonist. Furthermore, Tetrahydroberberine inhibits the DA-induced K+ current non-competitively in single dissociated cells, implying that Tetrahydroberberine may exhibit other pharmacological action on the central nervous system.
Zhongguo Yao Li Xue Bao. 1994 Mar;15(2):133-5.
Inhibitory effect of tetrahydroberberine on platelet aggregation and thrombosis.[Pubmed:
8010106]
METHODS AND RESULTS:
Tetrahydroberberine (THB), an alkaloid extracted from Corydalis ambigua, inhibited the rabbit platelet aggregation triggered by arachidonic acid (AA), ADP, and collagen with IC50 of 0.86, 1.31, and 1.10 mmol.L-1, respectively. Tetrahydroberberine reduced the thromboxane B2 (TXB2) generation in rabbit platelet-rich plasma triggered by AA. Tetrahydroberberine 30 mg.kg-1.d-1 ip for 3 or 5 d restrained the ADP-induced platelet aggregation in rats. Tetrahydroberberine 30 mg.kg-1.d-1 ip for 1, 3, or 5 d inhibited the AA-induced platelet aggregation in rats. Tetrahydroberberine 15-30 mg.kg-1 iv showed an inhibition of venous thrombosis in rats.
CONCLUSIONS:
The results show that Tetrahydroberberine is a potent inhibitor of platelet aggregation in vitro and in vivo and is a promising antithrombotic drug.
