Nitenin analogue compounds and their use in the treatment of chronic and acute pain

The present disclosure relates to nitenin analogue compounds (of formulas I, II, III and IV) and their use as pharmaceutical agent in the treatment, prevention or reduction of both acute and chronic pain. The mode of action disclosed herein allows nitenin and nitenin analogue compounds to act as ana...

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Hauptverfasser: LOPES DE SOUSA Marisa Isabel, DA SILVEIRA MAXIMO Patricia Isabel, PINTO FERREIRA Luisa Maria, SOVELA MOURAO Henrique, SZWARC DOS SANTOS Beatriz, SEGAO MONDRAGAO Miguel Angelo, DOS SANTOS BALTAZAR DE LIMA Pedro Afonso, FERREIRA DA COSTA LOURENCO Ana Maria, GOMES Rui, ROSADO SABINO Vanessa Alexandra, MACO ABREU Ana Rosa, HIM TONG Ming, PINHEIRO BASTOS Andre Emanuel, CLAUDETREMBLEAU Laurent Alain, MONTEIRO SERRAO Joana Maria, PENA LINO Silvia Patricia, DE SERIO BRANCO Paula Cristina
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creator LOPES DE SOUSA Marisa Isabel
DA SILVEIRA MAXIMO Patricia Isabel
PINTO FERREIRA Luisa Maria
SOVELA MOURAO Henrique
SZWARC DOS SANTOS Beatriz
SEGAO MONDRAGAO Miguel Angelo
DOS SANTOS BALTAZAR DE LIMA Pedro Afonso
FERREIRA DA COSTA LOURENCO Ana Maria
GOMES Rui
ROSADO SABINO Vanessa Alexandra
MACO ABREU Ana Rosa
HIM TONG Ming
PINHEIRO BASTOS Andre Emanuel
CLAUDETREMBLEAU Laurent Alain
MONTEIRO SERRAO Joana Maria
PENA LINO Silvia Patricia
DE SERIO BRANCO Paula Cristina
description The present disclosure relates to nitenin analogue compounds (of formulas I, II, III and IV) and their use as pharmaceutical agent in the treatment, prevention or reduction of both acute and chronic pain. The mode of action disclosed herein allows nitenin and nitenin analogue compounds to act as analgesic through reduction of K30 currents rather than their potentiation. Related to their high efficacy in the treatment of pain, these compounds are highly selective for slow voltage-activated potassium (K30 ) currents expressed in the small diameter dorsal root neurons (sDRGns), mainly on those mediated by the voltage-dependent potassium channel (KV), KV1.3. Such findings, together with those showing that nitenin and nitenin analogue compounds act as activity dependent blockers also lead to very reduced side-effects. The results disclosed herein show that nitenin and nitenin analogue compounds described herein are a viable alternative to the already existing pharmaceutical compounds used in the treatment of pain.
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title Nitenin analogue compounds and their use in the treatment of chronic and acute pain
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