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Discovery of δ Opioid Receptor Full Inverse Agonists and Their Effects on Restraint Stress-Induced Cognitive Impairment in Mice.
Hirayama, Shigeto; Iwai, Takashi; Higashi, Eika; Nakamura, Minami; Iwamatsu, Chiharu; Itoh, Kennosuke; Nemoto, Toru; Tanabe, Mitsuo; Fujii, Hideaki.
Afiliación
  • Hirayama S; Laboratory of Medicinal Chemistry, School of Pharmacy , Kitasato University , 5-9-1, Shirokane, Minato-ku, Tokyo 108-8641 , Japan.
  • Iwai T; Medicinal Research Laboratories, School of Pharmacy , Kitasato University , 5-9-1, Shirokane, Minato-ku, Tokyo 108-8641 , Japan.
  • Higashi E; Medicinal Research Laboratories, School of Pharmacy , Kitasato University , 5-9-1, Shirokane, Minato-ku, Tokyo 108-8641 , Japan.
  • Nakamura M; Laboratory of Pharmacology, School of Pharmacy , Kitasato University , 5-9-1, Shirokane, Minato-ku, Tokyo 108-8641 , Japan.
  • Iwamatsu C; Laboratory of Medicinal Chemistry, School of Pharmacy , Kitasato University , 5-9-1, Shirokane, Minato-ku, Tokyo 108-8641 , Japan.
  • Itoh K; Laboratory of Pharmacology, School of Pharmacy , Kitasato University , 5-9-1, Shirokane, Minato-ku, Tokyo 108-8641 , Japan.
  • Nemoto T; Laboratory of Medicinal Chemistry, School of Pharmacy , Kitasato University , 5-9-1, Shirokane, Minato-ku, Tokyo 108-8641 , Japan.
  • Tanabe M; Laboratory of Medicinal Chemistry, School of Pharmacy , Kitasato University , 5-9-1, Shirokane, Minato-ku, Tokyo 108-8641 , Japan.
  • Fujii H; Medicinal Research Laboratories, School of Pharmacy , Kitasato University , 5-9-1, Shirokane, Minato-ku, Tokyo 108-8641 , Japan.
ACS Chem Neurosci ; 10(5): 2237-2242, 2019 05 15.
Article en En | MEDLINE | ID: mdl-30913383
ABSTRACT
The cyclopropylmethyl group in classical δ opioid receptor (DOR) antagonist NTI, BNTX, and NTB was replaced with various electron-withdrawing groups to develop DOR inverse agonists. N-Benzyl NTB derivative SYK-657 was a potent DOR full inverse agonist and its potency was over 10-fold potent than that of a reference compound ICI-174,864. Intraperitoneal administration of SYK-657 induced the short-term memory improving effect in mice without abnormal behaviors.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Conducta Animal / Cognición / Receptores Opioides delta / Disfunción Cognitiva / Analgésicos Opioides / Memoria a Corto Plazo Límite: Animals Idioma: En Revista: ACS Chem Neurosci Año: 2019 Tipo del documento: Article País de afiliación: Japón
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Conducta Animal / Cognición / Receptores Opioides delta / Disfunción Cognitiva / Analgésicos Opioides / Memoria a Corto Plazo Límite: Animals Idioma: En Revista: ACS Chem Neurosci Año: 2019 Tipo del documento: Article País de afiliación: Japón