Rotundine(10097-84-4)

Analgesics: Rotundine, also known as craniodynine, levo-tetrahydropalmatine, chemical name is 2,3,9,10-tetrahydroxy-5,8,13,13a-tetrahydro-6H-dibenzo [a, g] quinazine, which is the left-handed substance of tetrahydropalmatine (dl-THP), is a blocker of dopamine receptor in the brain, preferentially blocks brain areas rich in dopamine receptor, such as cortex and striatum, and achieves analgesic effect by strengthening the function of internal anti-pain system and inhibiting the transmission of pain information to the center. Its analgesic effect is weaker than that of pethidine and stronger than that of general analgesics. It has no respiratory inhibition under the treatment dose, does not cause gastrointestinal smooth muscle spasm, and has certain effects on acute and chronic persistent pain and visceral blunt pain. It was first listed in China in 1985 and is applicable to patients suffering from insomnia due to pain. It can also be used for stomach ulcer and duodenal ulcer pain, menstrual pain, uterine contraction pain after delivery, tension insomnia, spastic cough, etc.

Character: white or yellowish flaky or columnar crystal, odorless, slightly bitter taste, yellow color when exposed to light and heat. It is insoluble in water, slightly soluble in ethanol, and easily soluble in chloroform and ether. Its solubility in sulfuric acid brine is large, and it is mostly made into injection.

Pharmacological action 1. Effect on the central nervous system (1) Analgesic, sedative, hypnotic and tranquilizing effects. Its analgesic effect is weaker than pethidine and stronger than general antipyretic and analgesic drugs. There is no respiratory inhibition and gastrointestinal smooth muscle spasm under the treatment dose. It has good effect on chronic persistent pain and visceral dull pain, but poor effect on polar sharp pain and advanced cancer pain. It can cause sedation and hypnosis while producing analgesic effect. The mechanism of action of rotundine remains to be elucidated, which may be related to the activation of this system by inhibiting the ascending of the brainstem reticular structure and blocking the function of multiple case-handling receptors in the brain. The amount of treatment is not addictive. (2) Rotundine can reduce the grade index of behavioral sensitization in rats and block the generation of behavioral sensitization in rats. 2. Effect on cardio-cerebrovascular system (1) Protective effect on cerebral ischemia-reperfusion injury Rotundine can significantly prolong the survival time of mice with cerebral ischemia, enhance the activities of superoxide dismutase and lactate dehydrogenase in brain tissue, and reduce the content of malondialdehyde and nitrogen monoxide, the products of lipid peroxidation in brain tissue. (2) Effects on myocardial ischemia-reperfusion injury: ligate the left anterior descending coronary artery of dogs for 40 minutes, and then conduct experimental study after reperfusion for 40 minutes. Rotundine can significantly reduce the incidence of ischemia-reperfusion ventricular arrhythmias, plasma norepinephrine concentration and serum creatine phosphokinase activity. (3) The experimental study on the effect of rotundine on cardio-cerebrovascular system showed that rotundine could significantly reduce the arterial blood pressure of rats in a dose-dependent manner, and the blood pressure was accompanied by a temporary slowing of heart rate. (4) Reversing the drug resistance of tumor cells, rotundine can significantly reverse the effect of multidrug resistance (MDR) of human breast cancer cell MCF-7. Its mechanism is related to the overexpression of P-glycoprotein (P-gp) in cells. Rotundine can reverse the drug resistance by downregulating the expression of P-gp in tumor cells and up regulating the expression of Topo Ⅱ. (5) The study of calcium antagonistic effect shows that rotundine can reduce the calcium channel current of guinea pig ventricular myocytes, prolong the recovery time of calcium channel, and have a tension-blocking effect on calcium channel and use dependence. (6) Effect on the endocrine system Rotundine can promote the secretion of pituitary adrenocorticin and excite the pituitary-adrenal system.

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