Inhibition of FAAH, TRPV1, and COX2 by NSAID-serotonin conjugates.

Rose, Tyler M; Reilly, Christopher A; Deering-Rice, Cassandra E; Brewster, Clinton; Brewster, Chelsea

Rose, Tyler M; Reilly, Christopher A; Deering-Rice, Cassandra E; Brewster, Clinton; Brewster, Chelsea.

Afiliação

Rose TM; Roseman University of Health Sciences, College of Pharmacy, 10920 South River Front Parkway, South Jordan, UT 84095, USA. Electronic address: trose@roseman.edu.
Reilly CA; University of Utah, College of Pharmacy, Department of Pharmacology and Toxicology, Salt Lake City, UT 84112, USA.
Deering-Rice CE; University of Utah, College of Pharmacy, Department of Pharmacology and Toxicology, Salt Lake City, UT 84112, USA.
Brewster C; Roseman University of Health Sciences, College of Pharmacy, 10920 South River Front Parkway, South Jordan, UT 84095, USA.
Brewster C; Roseman University of Health Sciences, College of Pharmacy, 10920 South River Front Parkway, South Jordan, UT 84095, USA.

Bioorg Med Chem Lett ; 24(24): 5695-5698, 2014 Dec 15.

Article em En | MEDLINE | ID: mdl-25467164

ABSTRACT

ABSTRACT

Serotonin was linked by amidation to the carboxylic acid groups of a series of structurally diverse NSAIDs. The resulting NSAID-serotonin conjugates were tested in vitro for their ability to inhibit FAAH, TRPV1, and COX2. Ibuprofen-5-HT and Flurbiprofen-5-HT inhibited all three targets with approximately the same potency as N-arachidonoyl serotonin (AA-5-HT), while Fenoprofen-5-HT and Naproxen-5-HT showed activity as dual inhibitors of TRPV1 and COX2.

Assuntos

Amidoidrolases/antagonistas & inibidores; Anti-Inflamatórios não Esteroides/química; Anti-Inflamatórios não Esteroides/farmacologia; Ciclo-Oxigenase 2/química; Serotonina/química; Canais de Cátion TRPV/antagonistas & inibidores; Flurbiprofeno/química; Flurbiprofeno/metabolismo; Humanos; Serotonina/metabolismo

Palavras-chave

Arachidonoyl serotonin; Dual inhibition; FAAH; Fatty acid amide hydrolase; Multimodal inhibition; NSAID; TRPV1; Transient receptor potential vanilloid type 1

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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Serotonina / Anti-Inflamatórios não Esteroides / Ciclo-Oxigenase 2 / Canais de Cátion TRPV / Amidoidrolases Limite: Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2014 Tipo de documento: Article

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