Metabolism of dynorphin A(1-13).

Brugos, B; Hochhaus, G

Brugos, B; Hochhaus, G.

Afiliación

Brugos B; Department of Pharmaceutics, College of Pharmacy, University of Florida, Gainesville 32610, USA.

Pharmazie ; 59(5): 339-43, 2004 May.

Article en En | MEDLINE | ID: mdl-15212298

RESUMEN

Dynorphin A(1-13), a tridecapeptide of the endogenous opioid peptides, has modest effects in reducing mild opiate withdrawal in humans. Previous studies revealed that dynorphin also potentiates the analgesic effect of morphine in morphine-tolerant rats and mice. The therapeutic potential of dynorphin A(1-13) is limited due to extensive metabolism by human metabolic enzymes resulting in an in vivo half-life of less than one minute. Chemical modifications of dynorphin A(1-13), such as N-methylation of Tyr1 and amidation of the C-terminus have been shown to be effective in protecting against the proteolytic enzymes in human plasma. This article is a general review of the metabolism of dynorphin A(1-13) in human plasma and CSF.

Asunto(s)

Dinorfinas/metabolismo; Fragmentos de Péptidos/metabolismo; Animales; Barrera Hematoencefálica; Dinorfinas/sangre; Dinorfinas/líquido cefalorraquídeo; Humanos; Fragmentos de Péptidos/sangre; Fragmentos de Péptidos/líquido cefalorraquídeo

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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Fragmentos de Péptidos / Dinorfinas Límite: Animals / Humans Idioma: En Revista: Pharmazie Asunto de la revista: FARMACIA Año: 2004 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Alemania

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