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CAS NO.42971-09-5
98%(1-25)Kilogram98%(26-500)Kilogram98%(501-1000)Kilogram
Vinpocetine
CAS: 42971-09-5;80038-06-8
Molecular Formula: C22H26N2O2
| Molecular Formula | C22H26N2O2 |
| Molar Mass | 350.46 |
| Density | 1.1260 (rough estimate) |
| Melting Point | 147-153 °C dec. |
| Boling Point | 484.44°C (rough estimate) |
| Specific Rotation(α) | D20 +114° (c = 1 in pyridine) |
| Flash Point | 207.506°C |
| Solubility | Soluble in chloroform or 96% ethanol, almost insoluble in water. |
| Vapor Presure | 0mmHg at 25°C |
| Appearance | White fine powder |
| Color | white |
| Maximum wavelength(λmax) | ['315nm(EtOH)(lit.)'] |
| Merck | 14,9991 |
| pKa | 7.87±0.60(Predicted) |
| Storage Condition | Sealed in dry,2-8°C |
| Stability | Photosensitive |
| Sensitive | Sensitive to light |
| Refractive Index | 1.6500 (estimate) |
| MDL | MFCD00211233 |
| Physical and Chemical Properties | White crystalline powder, odorless and tasteless. Soluble in chloroform or 96% ethanol, a few insoluble in water. Melting point 147-153 °c (decomposition). [Α] D20 +114 °(C = 1, pyridine). UV maximum absorption (96% ethanol):229,275,315nm (h28200, 12000,7100). Acute toxicity LD50 mice, rats (mg/kg):534,503 oral; 240,133.8 intraperitoneal injection; 58.7,42.6 intravenous injection. |
| Use | Cerebrovascular medication |
| cerebral vasodilator | vinpocetine is a cerebral vasodilator, which has a stronger effect than vinblastamide and selectively increases cerebral blood flow; it can increase and Improve the supply of cerebral oxygen, promote metabolism, enhance the deformability of red blood cells, reduce blood viscosity, inhibit platelet aggregation, and improve brain tissue metabolism. Mainly used to treat sequelae of cerebral infarction, sequelae of cerebral hemorrhage, cerebral arteriosclerosis, etc. It is also used to treat retinal vascular sclerosis and vasospasm, deafness and vertigo in the elderly. Vinpocetine is a semi-synthetic vincamine derivative. The effect is similar to that of vincamine, and it has a higher selective dilation effect on cerebral blood vessels. The pharmacological effects are as follows: ① Inhibit calcium-dependent phosphodiesterase activity, increase the cAMP content of relaxing vascular smooth muscle, thereby relaxing vascular smooth muscle and increasing cerebral blood flow. ②Enhance red blood cell deformability, reduce blood viscosity, inhibit platelet aggregation, thereby improving blood fluidity and microcirculation. (3) Promote the uptake of glucose in brain tissue and promote the metabolic transformation of monoamines in brain. ④ During cerebral ischemia, it can inhibit the increase of lactic acid in the brain, increase the content of ATP, inhibit the production of lipid peroxides in the brain, and delay the occurrence time of cerebral ischemia spasm, so it can improve brain metabolism and protect brain function. Figure 1 is a vinpocetine structure. |
| Application | Vinpocetine is often used for cerebral arteriosclerosis, cerebral ischemia and hemorrhagic stroke sequelae, transient ischemic attack and other cerebral circulation disorders It is also used to treat symptoms induced by cerebral circulation disorders, such as aphasia, inability to use, poor memory, cognitive dysfunction, dizziness, headache and other brain vestibular problems, etc, it is a first-line drug widely used in the treatment and prevention of ischemic cerebrovascular diseases. |
| Pharmacokinetics | Vinpocetine has high fat solubility, is easy to be absorbed by tissues, and is widely distributed. It can pass through the blood-brain barrier and is mainly metabolized in the liver. It is apovincamine, which is excreted by the kidney. |
| Efficacy and Function | Vinpocetine, also known as vinpac ethyl ester, Kangweinao, Karan, and ethyl apvinamide, is a natural medicine extracted from vinca vinca and belongs to indole alkaloids. Now it has been artificially synthesized. Its pharmacological effects: increase cerebral blood flow, increase the effect of cyclic guanosine by inhibiting Ca2 +-dependent phosphodiesterase activity, selectively relax smooth muscle, and increase cerebrovascular blood flow; improve blood fluidity and microcirculation, that is, by Enhancing the deformability of red blood cells, reducing blood viscosity, and inhibiting platelet aggregation to play this role; improving brain metabolism: increasing cerebral oxygen supply, promoting brain tissue uptake of glucose, and promoting brain monoamine metabolism and transformation, inhibit the increase of lactic acid metabolism and ATP content in ischemic brain, increase the oxygen dissociation degree of hemoglobin, increase the anti-hypoxia ability of brain, inhibit the occurrence of ischemic cerebral vasospasm and the production of lipid peroxides. It is well absorbed by oral administration, reaching a peak value at 1h, and metabolized into apovinylic acid in vivo. The plasma elimination half-life is about 1 hour. Continuous administration for 4 weeks, no accumulation in the body. Clinically used for clinical manifestations such as cerebral infarction sequelae, cerebral hemorrhage sequelae, cerebral arteriosclerosis, cerebral vasospasm, vertigo, tinnitus, headache, dizziness, numbness of the limbs, incontinence, and depression, Anxiety, sleep disorders and other mental symptoms. Clinical experience shows that it is effective regardless of the length of the disease and whether the symptoms are fixed. |
| indications | 1. neurology department: various cerebrovascular diseases and their sequelae, etc. 2. Department of Cardiology: Coronary heart disease, arteriosclerosis and abnormal blood viscosity. 3. Ophthalmology: visual impairment caused by poor blood circulation in various fundus, etc. 4. otonasal nuclei: hearing impairment, tinnitus, vestibular dysfunction, etc. 5. Neurosurgery: Rehabilitation treatment of brain function after various craniocerebral operations. |
| preparation method | at present, there are two preparation methods of vinpocetine, one is to carry out total synthesis by chemical method, and the other is to extract vinpocetine from plants containing vinpocetine as raw material for semi-synthesis. In the chemical synthesis of vinpocetine, the construction of the fifth ring occupies a key position, and there are many methods reported in the literature, such as Oppoleor aldehyde method, trimethylchlorosilane method, etc. |
| adverse reactions | the nervous system can see head weight, dizziness, occasional drowsiness and numbness of lateral limbs, etc. The digestive system can see nausea, vomiting, loss of appetite, abdominal pain, diarrhea, etc. The circulatory system can see symptoms such as facial flushing and dizziness. Leukopenia can be seen in the blood system. Liver reaction showed that AST and ALT increased, rare alkaline phosphatase increased. Renal reaction shows that blood urea nitrogen increases. Sometimes allergic reactions such as rash, urticaria, pruritus, etc. may occur, and the drug should be stopped at this time. Occasionally, slight decrease in blood pressure, tachycardia, etc. |
| precautions | patients with intracranial hemorrhage and pregnant or lactating women are prohibited. |
| use | an alkaloid extracted from Apocynaceae, a derivative of vincamine (Vincamine). Selective inhibition of cerebral vascular smooth muscle calcium-dependent phosphodiesterase, cGMP increase, cerebral vascular expansion, and then increase cerebral blood flow, improve cerebral circulation, but has little effect on cardiovascular and blood pressure. Fast onset, good tolerance, small adverse reactions. Used for dizziness, headache, memory impairment, mobility disorders, aphasia, hypertensive encephalopathy, etc., and also used for mental or neurological symptoms caused by cerebral blood circulation disorders. Cerebrovascular medication. Ca2 + calmodulin-dependent type I phosphodiesterase (PDE1) inhibitor A selective PDE1 inhibitor, IC50:21 μM, is also a pressure sensitive sodium ion channel. |
Mol Download Chemical properties
CAS:
42971-09-5
MF:
C22H26N2O2
MW:
350.46
EINECS:
256-028-0
MDL No.:
MFCD00211233
Melting point:
147-153 °C dec.
alpha
D20 +114° (c = 1 in pyridine)
Boiling point:
484.44°C (rough estimate)
Density
1.1260 (rough estimate)
refractive index
1.6500 (estimate)
storage temp.
Sealed in dry,2-8°C
solubility
DMSO: 5 mg/mL
pka
7.87±0.60(Predicted)
form
solid
color
white
optical activity
[α]/D 148.5±5.0°, c = 0.1 in chloroform
λmax
315nm(EtOH)(lit.)
Merck
14,9991
Stability:
Photosensitive
InChIKey
DDNCQMVWWZOMLN-IRLDBZIGSA-N
LogP
5.137 (est)
Xi'an Eastling biotech Co., Ltd. is dedicated to the research and development, production, and sales of natural plant extracts; With nearly 15 years of experience in identifying, researching, developing, and producing active ingredients for medicinal plants, we focus on providing innovative products and services to customers in industries such as pharmaceuticals, health food, and cosmetics.
Eastling Biotechnology has established a global direct harvesting system for plant raw materials, ensuring the high quality and authenticity of raw materials, while also protecting the continuity and diversity of plants; Having strong research and development capabilities, we can develop more effective and specialized plant active ingredients for the pharmaceutical, health food, and cosmetics industries; We have established an advanced quality control system, and the quality control of our products depends on advanced testing instruments and high-level technical experts. The effective combination of the two forms Eastling's ability to quickly and rigorously control product quality.
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