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Tetrahydropalmatine (THP) is a commonly used analgesic drug, mainly used for dull pain in the gastrointestinal and hepatobiliary systems, and pain during childbirth and dysmenorrhea. Its analgesic effect is not as good as morphine, but it is the best for chronic persistent dull pain, and the analgesic degree can reach 40% of morphine.
In addition, THP also has sedative and hypnotic effects and can be used for temporary insomnia. When using THP, the fetal ductus arteriosus needs to be monitored regularly to avoid adverse effects on the fetus.
Uses of tetrahydropalmatine.
Tetrahydropalmatine has analgesic, sedative, hypnotic and tranquilizing effects. Its analgesic effect is not as good as that of perthidine, but it is stronger than general antipyretic analgesics. DL-tetrahydropalmatine is the main active substance of the traditional Chinese medicine Corydalis yanhusuo, which can cause hypotension and bradycardia in rats by antagonizing striatal dopamine D2 receptors.
Preparation of tetrahydropalmatine.
A. Berberine hydrochloride is ring-opened in p-toluenesulfonic acid, xylene, HCl at 70°C to obtain demethylene berberine hydrochloride.
B. Demethylene berberine hydrochloride is methylated in potassium carbonate, methanol, dimethyl sulfate at 40°C to obtain palmatine hydrochloride.
C. Palmatine hydrochloride is racemized in methanol and sodium borohydride to obtain tetrahydropalmatine.
Product method of Bulk tetrahydropalmatine Powder.
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