Name | CYCLAZOSIN HYDROCHLORIDE |
Synonyms | CYCLAZOSIN HYDROCHLORIDE Cyclazosin monohydrochloride Cyclazosin Hydrochloride CDP Cyclazosin hydrochloride Solution Cyclazosin hydrochloride Solution, 100ppm 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(2-furanylcarbonyl) decahydroquinoxaline 2-[4-(furan-2-ylcarbonyl)octahydroquinoxalin-1(2H)-yl]-6,7-dimethoxyquinazolin-4-amine hydrochloride cis-1-(4-Amino-6,7-dimethoxy-2-quinazolinyl)-4-(2-furanylcarbonyl)decahydroquinoxaline monohydrochloride |
CAS | 146929-33-1 |
InChI | InChI=1/C23H27N5O4.ClH/c1-30-19-12-14-15(13-20(19)31-2)25-23(26-21(14)24)28-10-9-27(16-6-3-4-7-17(16)28)22(29)18-8-5-11-32-18;/h5,8,11-13,16-17H,3-4,6-7,9-10H2,1-2H3,(H2,24,25,26);1H |
Molecular Formula | C23H27N5O4 |
Molar Mass | 473.95 |
Boling Point | 691.1°C at 760 mmHg |
Flash Point | 371.7°C |
Solubility | H2O: 1.8mg/mL |
Vapor Presure | 2.43E-19mmHg at 25°C |
Appearance | solid |
Color | white |
Physical and Chemical Properties | Solubility: H2O: 1.8 mg/mL WGK Germany:3 |
WGK Germany | 3 |
indications | The main indications are consciousness disorders after acute craniocerebral surgery and brain surgery; clinically, it is also used for other functional and consciousness disorders caused by acute injury of the central nervous system, tremor paralysis, tinnitus and neurological deafness, sleeping pills Poisoning, etc.; in recent years, it has been widely used clinically for ischemic stroke, cerebral arteriosclerosis, multi-infarct dementia, Alzheimer's disease, pediatric viral encephalitis, etc. |
action | citicoline (Citicoline) is an endogenous nucleoside naturally produced in vivo and is an intermediate of the main pathway of phospholipid biosynthesis in cell membrane. The repair of nerve cell membranes requires a large amount of citicoline. Supplementation of exogenous citicoline can promote the synthesis of phospholipids in nerve cell membranes. Citicoline plays an extremely important role in maintaining a variety of cellular physiological processes. In a variety of cell membrane dysfunction and degenerative diseases caused by ischemia and hemorrhage, citicoline has obvious clinical therapeutic effect. |
Citicoline is a nucleic acid derivative, which plays an important role in the synthesis of lecithin and improves brain function by promoting the synthesis of lecithin. Compared with other neuroprotective drugs, citicoline has stronger evidence-based medicine and is more widely used in clinical practice. The drug was first developed by Takeda Company of Japan in 1967, and its trade name is Nicolin. It has been clinically applied for nearly half a century. He officially entered our country in 1988.
The bioavailability and pharmacokinetic characteristics of the oral dosage form of citicoline are similar to those of intravenous medication. The oral absorption is complete, and the oral dosage form is more conducive to the long-term medication of patients, which can bring greater benefits to patients and is very popular in clinical practice.
Citicoline is mainly used in the clinical treatment of stroke, cerebral edema, head injury, vertigo, encephalitis neuritis, senile dementia and consciousness disorders caused by various nerve injuries. Most of these diseases have a long recovery period and require long-term medication. The use of injections is extremely inconvenient, and oral preparations have long been recognized by doctors and patients due to their advantages of convenience, safety and effectiveness.
nucleic acid derivatives | citicoline is a nucleic acid derivative, which plays an important role in the synthesis of lecithin and improves brain function by promoting the synthesis of lecithin. Compared with other neuroprotective drugs, citicoline has stronger evidence-based medicine and more extensive clinical application. The drug was first developed by Takeda Company of Japan in 1967, and its trade name is Nicolin. It has been clinically used for nearly half a century. He officially entered our country in 1988. The bioavailability and pharmacokinetic characteristics of the oral dosage form of citicoline are similar to those of intravenous medication. The oral absorption is complete, and the oral dosage form is more conducive to the long-term medication of patients, which can bring greater benefits to patients, and is very popular in clinical practice. Citicoline is mainly used clinically for the treatment of stroke, cerebral edema, craniocerebral injury, vertigo, encephalitis neuritis, senile dementia and consciousness disorders caused by various nerve injuries. Most of these diseases have a long recovery period and require long-term medication. The use of injections is extremely inconvenient, and oral preparations have long been recognized by doctors and patients due to their advantages of convenience, safety and effectiveness. |
pharmacology | citicoline (C14H26N4O11P2) is a single nucleotide derivative composed of nucleic acid, cytosine, pyrophosphate and choline. Oral administration can be quickly absorbed and hydrolyzed into choline and cytosine in the intestine and liver. The latter two enter the blood circulation system, cross the blood-brain barrier, and recombine into citicoline in the central nervous system. The synthesis of 80% phospholipids in the central nervous system is affected by the concentration of citicoline in the body. In addition, citicoline can be converted into acetylcholine in the central nervous system and oxidized to betaine in the kidney and liver. Citicoline has good water solubility and bioavailability as high as 90%. Only less than 1% is excreted in feces after oral administration. There are 2 absorption peaks in plasma, 1 h and 24 h after ingestion. In the rat model, after 10 hours of ingestion of radiolabeled citicoline, its content steadily increased in the brain and was widely distributed in the white and gray matter of the brain. The high concentration remained at the 48th hour, and its elimination was very slow. Only a small amount was excreted through urine, feces and breathing every day. Exogenous intake of citicoline can promote the rapid repair of damaged cell surface and mitochondrial membrane, maintain cell integrity and biological performance, and inhibit cell apoptosis and death. |
indications | the main indications are consciousness disorders after acute brain surgery and brain surgery; clinically, it is also used for other functional and conscious disorders caused by acute injuries of the central nervous system, tremor paralysis, tinnitus and neurological deafness, sleeping drug poisoning, etc; in recent years, it has been widely used clinically for ischemic stroke, cerebral arteriosclerosis, multi-infarct dementia, Alzheimer's disease, viral encephalitis in children, etc. |
action | citicoline (Citicoline) is an endogenous nucleoside naturally produced in the body and an intermediate of the main pathway of cell membrane phospholipid biosynthesis. The repair of nerve cell membranes requires a large amount of citicoline. Supplementation of exogenous citicoline can promote the synthesis of phospholipids in nerve cell membranes. Citicoline plays an extremely important role in maintaining a variety of cellular physiological processes. In a variety of cell membrane dysfunction and degenerative diseases caused by ischemia and hemorrhage, citicoline has obvious clinical therapeutic effect. |
use | citicoline can restore the structure of cell membrane after brain cell injury, enhance the function of cell membrane and improve the function of neurons; 2. it can reduce cerebrovascular resistance, increase cerebral blood flow, promote brain metabolism, improve cerebral circulation and improve brain function; 3. It can increase the secretion of neurotransmitters including acetylcholine and dopamine, enhance the function of the brainstem reticular structure related to consciousness, improve the body's state of consciousness, and increase the speed of awakening; 4. It can also inhibit phospholipase A2 Activation, thereby accelerating the reabsorption of cerebral edema. 5. It can enhance dopaminergic activity and regulate the physiological function of extrapyramidal system. 6. It has been proved to have the function of increasing memory and promoting learning. |