Idebenone (IDBN), also known as 6- (10-hydroxydecyl) -2,3-dimethoxy-5-methylbenzoquinone, is an intelligent promoter drug developed and marketed by Takeda Pharmaceutical Co., Ltd. in Japan in 1986; It has an activating effect on the function of the body, improves brain metabolism and functional impairment, and can increase the utilization rate of glucose in the brain, promoting ATP generation; Improving the metabolism of the neurotransmitter serotonin in the brain, it has strong antioxidant and free radical scavenging effects. In clinical practice, it is mainly used to treat many central nervous system degenerative diseases related to oxidative stress, such as Parkinson's disease, Alzheimer's disease, multi infarct dementia, local cerebral anemia, and brain failure. It is also used for the treatment of Friedrichshafen ataxia and can be used in cosmetic formulations. It has cosmetic efficacy in clearing free radicals, inhibiting lipid peroxidation, suppressing inflammation, inhibiting DNA damage, photoprotection, reducing pigmentation, etc.

Physical and chemical properties

Adibenone is a yellow crystalline or crystalline powder, odorless. Extremely insoluble in water, highly soluble in chloroform, methanol or anhydrous ethanol, soluble in ethyl acetate, and insoluble in n-hexane.

market conditions

Idebenone was first developed by Takeda Pharmaceutical Co., Ltd. in Japan. In 2005, Santhera Pharmaceuticals in Switzerland and Takeda Pharmaceuticals in Japan announced their joint research and development of idebenone for the treatment of FRDA (Friedrichshafen ataxia), and it became the first therapeutic drug for FRDA, marking that the drug had entered the mature stage. Edebenone has an activating effect on mitochondrial function, improves brain energy metabolism and functional impairment, enhances glucose utilization in the brain, promotes ATP production, improves the metabolism of neurotransmitter 5-hydroxytryptamine in the brain, and has strong antioxidant and free radical scavenging effects. The anti-aging experiment conducted by the anti-aging association of Virginia in the United States has proved that its anti-oxidation effect is better than that of common antioxidants on the market, such as vitamin E, coenzyme Q10 and vitamin C. Studies have shown that idebenone can promote intelligent rehabilitation and improve the quality of life of patients with vascular dementia, and its short-term efficacy is better than that of nifedipine.

Pharmacology

This product is a medication for improving brain metabolism and mental symptoms. It can activate the respiratory activity of brain mitochondria, improve brain energy metabolism disorders, and alleviate neurological symptoms, emotional disorders, and passive avoidance response disorders in stroke and experimental ischemic animals.

1. Improvement effect on cerebral dysfunction during cerebral ischemia: 

① This product has an improvement effect on post-stroke residual symptoms, emotional disorders (reduced spontaneous movement, increased susceptibility to stimulation), limb paralysis, etc. in spontaneously hypertensive rats (SHRSP) prone to stroke. 

② It can improve passive avoidance response disorders in rats with experimental cerebral infarction, experimental transient cerebral ischemia, and bilateral basal forebrain damage This product can delay the onset and death time of spasms in SHRSP with bilateral carotid artery ligation, and also delay the death time of hypoxemic mice It has an improving effect on the decreased acetylcholine content and 5-hydroxytryptamine metabolism update in the brain of experimental transient cerebral ischemia rats, and can increase monoamine metabolites in the cerebrospinal fluid of patients with cerebrovascular disorders.

2. Improvement effect on brain energy metabolism disorders during cerebral ischemia: 

① It has an inhibitory effect on the decrease of ATP and increase of lactate in the brain of SHRSP with bilateral common carotid artery ligation and experimental transient cerebral ischemia rats. 

② This product can restore the low glucose utilization rate in the brains of rats with SHRSP stroke and damage to the basal ganglia.

3. Activation effect on respiratory activity of brain mitochondria: 

① Succinic acid and NADH oxidase activity (respiratory activity) can be restored in injured dog brain mitochondrial samples in vitro, which can activate the electron transport system function of rat brain mitochondria.

 ② In vivo, it can inhibit the production of peroxidized lipids by rat and dog brain mitochondria, prevent mitochondrial membrane disorders (swelling) associated with peroxidized lipid production, and maintain their function.

clinical application

1. Used to treat many central nervous system degenerative diseases related to oxidative stress, such as Parkinson's disease, Alzheimer's disease, multi infarct dementia, local cerebral anemia, and brain failure.

2. Used for the treatment of Friedreich's ataxia.

3. Treat cardiovascular and cerebrovascular diseases.

Overview, physicochemical properties, preparation methods, and clinical applications of idebenone. (2015-11-19)

Purpose:

Brain function improver can improve the metabolism of brain energy, enhance brain function, and have a mild antihypertensive effect. Clinically used for patients with brain dysfunction, low consciousness, emotional disorders, language disorders, dementia, etc. caused by cerebral infarction, cerebral hemorrhage, and sequelae of arteriosclerosis.

Idebenone belongs to the central nervous system stimulants and is used as a brain circulation improvement drug and intelligent promotion drug.