126580-45-8Relevant articles and documents
Discovery of δOpioid 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
, p. 2237 - 2242 (2019)
The cyclopropylmethyl group in classical δopioid 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.