2-AMINO-6-[[(4-FLUOROPHENYL)METHYL]AMINO]-3-PYRIDINYL]-CARBAMIC ACID, ETHYL ESTER MALEATE;Flupirtinemaleatelupirtine;Ethyl-2-amino-6-[(4-fluorbenzyl)amino]pyridin-3-carbamat, Verbindung mit Maleinsure (1:1);Keiton;Ketadolon;Flupirtine Maleate Salt;2-AMino-6-[(p-fluorobenzyl)aMino]-3-pyridinecarbaMic Acid Ethyl Ester Maleate;N-[2-AMino-6-[[(4-fluorophenyl)Methyl]aMino]-3-pyridinyl]carbaMic Acid Ethyl Ester (2Z)-2-Butenedioate
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.
Flupirtine maleate is a centrally-acting, non-addicting analgesic agent somewhat more potent than aspirin, paracetamol and pentazocine. It is reported to be useful in the treatment of postoperative and dental pain.
Flupirtine is an activator of voltage-gated potassium channel 7 (Kv7/KCNQ). It induces relaxation of preconstricted pulmonary arteries isolated from wild-type and serotonin transporter-overexpressing (SERT+) mice. Flupirtine (30 mg/kg per day) decreases mean right ventricular pressure and right ventricular hypertrophy in hypoxia-induced and SERT+ mouse models of pulmonary arterial hypertension. It increases the paw withdrawal threshold in a rat model of streptozotocin-induced diabetic neuropathy when administered at a dose of 10 mg/kg and increases paw withdrawal latency in a rat model of carrageenan-induced paw inflammation when used in combination with morphine. Flupirtine also indirectly antagonizes NMDA receptors via its effects on potassium channels.
Analgesic. Substituted pyridine with central analgesic properties. A potassium channel opener.
Analgesic. Substituted pyridine with central analgesic properties.
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