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Flupirtine maleate

Description Painkiller References
Flupirtine maleate
Flupirtine maleate
CAS No.
75507-68-5
Chemical Name:
Flupirtine maleate
Synonyms
Keiton;W 2964M;Ketadolon;Flupirtine Maleat;Fluoxetine Maleate;FLUPIRTINE MALEATE;Flupirtine Maleate Salt;Flupirtine maleate, >=99%;Flupirtinemaleatelupirtine;Flupirtine Maleate-001-salt
CBNumber:
CB2805021
Molecular Formula:
C19H21FN4O6
Formula Weight:
420.3916432
MOL File:
75507-68-5.mol

Flupirtine maleate Properties

Melting point:
186-188°C
storage temp. 
2-8°C
solubility 
DMSO: soluble >20mg/mL
form 
solid
color 
white
λmax
343nm(CH3CN)(lit.)
Merck 
14,4190
InChIKey
DPYIXBFZUMCMJM-BTJKTKAUSA-N

SAFETY

Safety Statements  22-24/25-35-20
WGK Germany  3
RTECS  EY8555800
HS Code  29333990

Flupirtine maleate price More Price(7)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich F8927 Flupirtine maleate salt ≥98% (HPLC) 75507-68-5 5mg $102 2018-11-20 Buy
Sigma-Aldrich F8927 Flupirtine maleate salt ≥98% (HPLC) 75507-68-5 25mg $348 2018-11-20 Buy
TCI Chemical F0736 Flupirtine Maleate Salt >98.0%(HPLC)(T) 75507-68-5 100mg $156 2018-11-22 Buy
TCI Chemical F0736 Flupirtine Maleate Salt >98.0%(HPLC)(T) 75507-68-5 1g $785 2018-11-22 Buy
Cayman Chemical 16674 Flupirtine (maleate) ≥95% 75507-68-5 25mg $29 2018-11-13 Buy

Flupirtine maleate Chemical Properties,Uses,Production

Description

Flupirtine is a selective neuronal potassium channel opener (SNEPCO) that also has N-methyl-D-aspartate (NMDA) receptor antagonist property which has been shown to be effective in the management of body pain. Flupirtine is used as an analgesic for acute pain, in moderate-to-severe cases. Its muscle relaxant properties make it popular for back pain and other orthopedic uses, but it is also used for migraines, in oncology, postoperative care, and gynecology. It is also effective in other painful conditions in which the primary requirement for analgesia is without sedation or anti-inflammatory effects.
It first became available in Europe in 1984 under the brand name Katadolon.
Flupirtine is a derivative of triaminopyridine with a chemical formula of ethyl-N-{2-amino-6-(4-fluorophenylmethylamino) pyridine-3 yl} cabamate. It is available as the maleate salt because flupirtine is itself poorly water soluble. Flupirtine is a base and is weakly lipophilic.

Painkiller

At present, the pain medications, used in the clinical in China, are divided into two categories: a class is to morphine on behalf of narcotic analgesics, and the other is aspirin antipyretic analgesics as representative. While the former high pain intensity, but addiction is its Achilles heel, which greatly limits its application; but the latter, although with no addictive analgesic strength, but it is weak, and has serious gastrointestinal effects.
Flupirtine Maleate, developed by Pliva,is subsidiary company German AWD, a new non-opioid analgesics central, listed in Germany in 1986 for the treatment of postoperative pain, dental pain, painful wounds and burns. Then in 1990, it was applied in the treatment of degenerative joint disease, neuropathic and cancer pain, migraine, headache and dysmenorrhea indications. After that, the flupirtine maleate list in Brazil and Portugal.
China approved the company's German AWD flupirtine maleate capsules imports in September in 2006, trade name: Kodak DoLong (Katadolon (R)).
Flupirtine maleate is a selective neuronal potassium channel opener, oral easily absorbed, which has three efficacy about analgesic, muscle relaxant and neuroprotective. It showed analgesic effects to pain caused by a variety of reasons. Flupirtine maleate has no affinity to Ah receptor, which do not inhibit prostaglandin synthesis. It is not antagonistic naloxone. Pain intensity (ED50) was weaker than methadone, buprenorphine and morphine, about 50% of morphine. Comparable to that of pentazocine, Flupirtine maleate is better than pethidine, codeine, phenacetin and paracetamol. Such as in the hot plate test, the effect of the strength of flupirtine (ED50 of 32mg/Kg, oral administration) is about half of morphine, codeine is 2 times, 10 times stronger than paracetamol and phenacetin. In the wake of dog dental pulp stimulation experiment, the analgesic intensity (ED50 of 3.5mg/ Kg, oral administration) is same with pentazocine.
Oral absorption of this product is about 90%, and rectal administration of this product is about 70%. After oral administration of 20~30min. It showed the pharmacological effects, and the duration of action is 3~5h. Plasma half-life is 8~11h. The drug is in the body tissues, mainly in the liver metabolism, and about 70% of the drug is eliminated by the kidneys. Flupirtine maleate is inhibited to pain caused by various diseases. the analgesic effect is between methadone and paracetamol. Centrally acting, but it did not inhibit the respiratory cardiovascular systems, and has no pharmacological activity impact for cough center, nor constipation and urinary retention. Long-term use does not produce tolerance and dependence. It has no painkillers side effects like other medicines on the market, such as addiction, gastrointestinal symptoms. Long term use after a few years the efficacy is not reduced, but can reduce the amount of taking. In short, flupirtine maleate has good clinical application prospect.

References

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3557425/
https://en.wikipedia.org/wiki/Flupirtine

Chemical Properties

Off-White Solid

Uses

Analgesic. Substituted pyridine with central analgesic properties.

Biological Activity

Non-opioid analgesic with muscle relaxant properties. Activates K + channels and indirectly antagonizes NMDA receptors. Exhibits neuroprotective actions in a model of cerebral ischemia in mice and reduces apoptosis and necrosis induced by noxious stimuli.

Flupirtine maleate Preparation Products And Raw materials

Raw materials

Preparation Products


Flupirtine maleate Suppliers

Global( 183)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 22049 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 20786 55
Mainchem Co., Ltd.
+86-0592-6210733
+86-0592-6210733 sales@mainchem.com CHINA 32651 55
Shanghai Yingrui Biopharma Co., Ltd.
+86-21-33585366 E-mail:sales03@shyrchem.com
+86-21-34979012 sales03@shyrchem.com CHINA 663 60
Hubei Jusheng Technology Co.,Ltd.
86-155-27864001
peter@hubeijusheng.com CHINA 18004 58
Jinan Tenglong Chemical Co.,Ltd
Whatsapp:+8615563263311 Skype:live:smions7080
smions7080@gmail.com CHINA 770 58
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 19990 58
hebei chisure biotechnology co.,ltd
0311 66567340
0311 66567340 admin@SpeedGainpharma.com CHINA 518 58
Hebei Ruishun Trade Co.,LTD
17052563120
Mike@rsbiology.com CHINA 300 58
Hebei Huanhao Biotechnology Co., Ltd.
86-0311-83975816
86-0311-83975816 lisa@hbhuanhao.com CHINA 668 58

View Lastest Price from Flupirtine maleate manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2018-12-17 Flupirtine maleate
75507-68-5
US $7.00 / kg 1kg 99% 100kg career henan chemical co
2018-11-06 API OF FLUPIRTINE MALEATE CAS 75507-68-5
75507-68-5
US $1.00 / KG 1KG 99% 20tons hebei chisure biotechnology co.,ltd
2018-11-05 good price flupirtine maleate CAS:75507-68-5
75507-68-5
US $1.00 / KG 1KG 99% 20ton hebei chisure biotechnology co.,ltd

75507-68-5(Flupirtine maleate)Related Search:


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