Praziquantel Cas 55268-74-1
1-a]-isoquinolin-4-one,2-(cyclohexylcarbonyl)-1,2,3,6,7,11b-hexahydro-4H-pyrazino-[2;2-cyclohexylcarbonyl-1,2,3,6,7,11b-hexahydro-4h-pyrazino(2,1-a)isoquinolin-4;4h-pyrazino(2,1-a)isoquinolin-4-one,2-(cyclohexylcarbonyl)-1,2,3,6,7,Chemicalbook11b-hexah;4H-pyrazino-[2,1-a]-isoquinolin-4-one,2-(cyclohexylcarbonyl)-1,2,3,6,7,11b-hexahydro-;biltricide;droncit;Praziquantelforsystemsuitability;2-(Cyclohexanecarbonyl)-1，3，4，6，7，11b-hexahydro-4H-pyrazino[2，1-α]isoquinolin-4-one
insecticide
praziquantel (praziquantel) is a broad spectrum insect repellent synthetic drug found abroad in the 1970s. After it was reported to be effective against schistosomiasis in 1977, it was trial-produced in China in the same year, and proved to be effective against schistosomiasis japonica. This product is colorless crystalline powder, odorless and slightly bitter, and stable under normal conditions. Soluble in chloroform, dimethyl sulfoxide and other organic solvents, slightly soluble in ethanol, difficult to dissolve in water. The histochemical results of in vivo and in vitro experiments showed that the glycogen, RNA and alkaline phosphatase were decreased, and the activity of alkaline protein reaction or acid phosphatase was increased.
Action mechanism
Praziquantel can kill adult schistosomiasis significantly. Its mechanism of killing insects, from the molecular level, is that praziquantel rapidly destroys the Ca2+ balance in the worm, on the one hand, it leads to the excitement of the worm body activity and muscle contracture, so that the parasitic schistosoma parasitic on the portal vein system can not be adsorbed on the blood vessel wall and is carried by the blood flow into the liver (liver migration), and then is damaged; Second, the syncytial cortex of schistosoma is damaged. In addition to affecting the absorption, excretion and secretion functions of the worm, resulting in the disturbance of glucose metabolism and enzyme system, the body surface antigen determining cluster of the worm is exposed, which can be recognized by the host immune system and attract a large number of inflammatory cells such as neutrophils, eosinophils and macrophages to gather around the worm and attack.
Side effect
The common side effects of praziquantel are as follows: 1. Dizziness, headache, nausea, abdominal pain, diarrhea, weakness, and limb soreness may occur 1 hour after the first use of praziquantel. Generally, the degree is mild, the duration is short, and the treatment is not affected. 2. Palpitations, chest tightness and other symptoms were observed in a few cases. Electrocardiogram showed T-wave changes and extrasystole, and occasionally supraventricular tachycardia and atrial fibrillation. 3, a few cases may appear transient aminotransferase elevation, toxic hepatitis, etc. 4, occasionally can induce mental disorders or gastrointestinal bleeding. 5, brain hernia, allergic reactions (rash, asthma) and so on have also been seen.
Chemical property
White or white crystalline powder, odorless, slightly bitter, hygroscopic. Solubility (g/100m1) : ethanol 9.7, chloroform 56.7, water 0.04. Soluble in dimethyl sulfoxide, insoluble in ether. Melting point 136 ~ 141℃. Acute toxicity LD50 mice and rats (mg/kg) : 2000 ~ 3000 orally, > 3000 subcutaneously.
use
Praziquantel is a broad-spectrum anti-parasitic drug, which is effective against Schistosoma japonicum, Schistosoma mansoni and Schistosoma Egyptii, clonorchis sinensis, pneumofluke, Zingiberum, tapeworm and cysticercus. In particular, it has a powerful killing effect on tapeworms, and is the best kind of schistosomiasis drugs at present.
