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AssigneeSea4US - Biotecnologia E Recursos Marinhos, Lda.
InventorsPedro Afonso Dos Santos Baltazar De Lima, Beatriz Szwarc Dos Santos, Ana Rosa Maço Abreu, AndréEmanuel Pinheiro Bastos, Marisa Isabel Lopes De Sousa, Joana Maria Monteiro Serrão, Patricia Isabel Da Silveira Maximo, Ana Maria Ferreira Da Costa Lourenco, Miguel Angelo Segão Mondragão
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The present patent application relates to the use of antagonists of delayed rectifier potassium (K+) channels, more specifically Kv1.3 antagonists, as pharmaceutical agents in the treatment, prevention or reduction of both acute and chronic pain. The results and mode of action disclosed herein describe how Kv1.3 antagonists may act as analgesics through reduction of K+ currents rather than their potentiation. With regard to their high efficacy in the treatment of pain, these compounds are highly selective for slow delayed rectifier voltage-activated potassium (K+) currents. Such findings, together with those showing that nitenin, PSORA-4, PAP-1 and AM92016 hydrochloride act as K+ channel blockers and by their effects on K+ current inactivation profiles, also translate into an analgesic effect with reduced side effects. The results disclosed herein show that compounds that inhibit delayed rectifying Kv1.3 channels, such as the ones described herein, are a viable alternative to the already existing pharmaceutical compounds used in the treatment of pain, and specially, in chronic pain.
An analgesic composition comprising a pharmacologically acceptable diluent or carrier and a therapeutically effective amount of one or more compounds that are antagonists of the slow delayed rectifier Kv1.3 channel, or pharmaceutical salts thereof, wherein the compound is an antagonist of the slow delayed rectifier Kv1.3 channel when the compound inhibits one or more slow delayed rectifier Kv1.3 channels, as evaluated by measuring the effect of the compound on slow delayed rectifier voltage-activated K+ currents recorded from small-diameter dorsal root neurons (DRG) neurons and/or small diameter trigeminal ganglia (TG) neurons;
A method of treating chronic pain or acute pain in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound that is an antagonist of the slow delayed rectifier Kv1.3 channel, or a pharmacologically acceptable salt thereof, wherein the compound is an antagonist of the slow delayed rectifier Kv1.3 channel when the compound inhibits one or more slow delayed rectifier Kv1.3 channels, as evaluated by measuring the effect of the compound on slow delayed rectifier voltage-activated K+ currents recorded from small-diameter dorsal root neurons (DRG) neurons and/or small diameter trigeminal ganglia (TG) neurons, wherein the compound is not AM92016 hydrochloride.
Dependencies are inferred from the claim text.