Rotundine Raw Materials Rotundine powder

CAS:10097-84-4

MF:C21H25NO4

MW:355.43

EINECS:1592732-453-0

Specification: 99% min Rotundine powder

Sample:Rotundine powder

Packaging:1kg/bag, 25kg/drum

Brand: Henrikang

Appearance: White

Storage: Cool Dry Place

Shelf Life: 2 Years

Test Method: HPLC

Rotundine powder Usage and Synthesis.

Rotundin, also known as cranial painkillers, levothyroxine, chemical name 2,3,9,10-tetramethoxy-5,8,13,13a-tetrahydro-6H-dibenzo[a,g]quinolizine, is the levothyroxine of DL-THP, is a dopamine receptor blocker in the brain, preferentially blocking the dopamine receptor-rich brain areas such as the cortex, It preferentially blocks brain areas rich in dopamine receptors, such as cortex and striatum, and achieves analgesia by strengthening the function of the intrinsic antinociceptive system and inhibiting the transmission of pain messages to the centre.

Its analgesic effect is weaker than pethidine, stronger than general analgesics, and in therapeutic doses without respiratory inhibition, does not cause gastrointestinal smooth muscle spasm, acute and chronic persistent pain and visceral dull pain have a certain effect.

Uses of Rotundine powder.

Used as an analgesic for headaches of the gastrointestinal tract and hepatobiliary system caused by internal diseases, dysmenorrhoea and pain relief in childbirth.

Physiological effect of Rotundine powder.

1. Effects on the central nervous system

(1) Analgesic, sedative, hypnotic and stabilising effects, its analgesic effect is weaker than pethidine, stronger than the general antipyretic and analgesic. Under the therapeutic dose, it has no respiratory inhibition and does not cause gastrointestinal smooth muscle spasm.

It is more effective in chronic persistent pain and visceral dull pain, and less effective in polar sharp pain and advanced cancer pain. In the production of analgesic effect at the same time, can cause sedation and hypnosis.

The mechanism of action of Rotundin is yet to be elucidated and may be related to the activation of this system through inhibition of the brainstem reticular formation upstream, blocking the function of the brain's multiple case receptors. The therapeutic amount is non-addictive.

(2)Anti-behavioural sensitisationRotundin can reduce the rank index of behavioural sensitisation in rats and block the production of behavioural sensitisation effect in rats.

2. Effects on cardio-cerebral vascular system

(1)Protective effect on cerebral ischemia/reperfusion injuryRotundin can significantly prolong the survival time of cerebral ischemia mice, enhance the activity of superoxide dismutase and lactate dehydrogenase in brain tissue, and reduce the content of malondialdehyde and nitric oxide, which are the products of lipid peroxidation in brain tissue.

(2)Effect on myocardial ischemia-reperfusion injury Ligation of the left anterior descending coronary artery of dogs for 40 minutes, followed by reperfusion for 40 minutes for experimental studies, Rotundin can significantly reduce the incidence of ischemia-reperfusion ventricular arrhythmia, plasma norepinephrine concentration and serum creatine phosphokinase activity.

(3) Cardiovascular effects of Rotundin can significantly reduce arterial blood pressure in rats in a dose-dependent relationship, accompanied by a transient slowing of the heart rate while lowering blood pressure.

Synthesis method of Bulk Rotundine powder.

Rotundin can be extracted from the tuberous roots of Hua Qian Jin Vine and Round Leaf Qian Jin Vine, etc., and the content of rotundin in plants of different origins ranges from about 0.01 per cent to 5.7 per cent. However, due to excessive logging, the plant resources have been seriously lacking. Therefore, chemical synthesis was used to prepare this drug.

The target compound Rotundin was obtained by a 3-step reaction of reduction, splitting and alkalisation, using xanthohumol as the starting material; and the tetrahydropalmatine dextrose was made into iodinated xanthohumol by alkalisation and oxidation, which can be used to prepare Rotundin repeatedly.