The MCH(1) receptor, an anti-obesity target, is allosterically inhibited by 8-methylquinoline derivatives possessing subnanomolar binding and long residence times.

Sakurai, T; Ogawa, K; Ishihara, Y; Kasai, S; Nakayama, M

Sakurai, T; Ogawa, K; Ishihara, Y; Kasai, S; Nakayama, M.

Afiliación

Sakurai T; Pharmaceutical Research Division, Takeda Pharmaceutical Company Limited, Kanagawa, Japan.

Br J Pharmacol ; 171(5): 1287-98, 2014 Mar.

Article en En | MEDLINE | ID: mdl-24670150

Asunto(s)

Fármacos Antiobesidad/farmacología; Benzamidas/farmacología; Quinolinas/farmacología; Receptores de Somatostatina/antagonistas & inhibidores; Regulación Alostérica; Animales; Células CHO; Cricetulus; Humanos; Receptores de Somatostatina/genética; Receptores de Somatostatina/metabolismo

Palabras clave

antagonist; melanin-concentrating hormone receptor 1 (MCH1 receptor); negative allosteric modulator; obesity; slow dissociation; time-dependent inhibition

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Texto completo: 1 Base de datos: MEDLINE Asunto principal: Quinolinas / Benzamidas / Receptores de Somatostatina / Fármacos Antiobesidad Idioma: En Revista: Br J Pharmacol Año: 2014 Tipo del documento: Article

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