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药效评价Spirocyclic delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-3-hydroxy-4-(spiro[chromene-2,4'-piperidine]-4-yl) benzamide (ADL5747).

期刊:Journal of medicinal chemistry发表年份:2009作者:Bertrand Le Bourdonnec; Rolf T Windh; Lara K Leister; Q Jean Zhou; Christopher W Ajello; Minghua Gu; Guo-Hua Chu; Paul A Tuthill; William M Barker; Michael Koblish; Daniel D Wiant; Thomas M Graczyk; Serge Belanger; Joel A Cassel; Marina S Feschenko;

药效评价The evolutionarily conserved residue A653 plays a key role in HERG channel closing.

期刊:The Journal of physiology发表年份:2009作者:Svetlana Z Stepanovic; Franck Potet; Christina I Petersen; Jarrod A Smith; Jens Meiler; Jeffrey R Balser; Sabina Kupershmidt

药效评价Design, synthesis, and biological evaluation of 6alpha- and 6beta-N-heterocyclic substituted naltrexamine derivatives as mu opioid receptor selective antagonists.

期刊:Journal of medicinal chemistry发表年份:2009作者:Guo Li; Lindsey C Aschenbach; Jianyang Chen; Michael P Cassidy; David L Stevens; Bichoy H Gabra; Dana E Selley; William L Dewey; Richard B Westkaemper; Yan Zhang

药效评价Identification of an orally active opioid receptor-like 1 (ORL1) receptor antagonist 4-{3-[(2R)-2,3-dihydroxypropyl]-2-oxo-2,3-dihydro-1H-benzimidazol-1-yl}-1-[(1S,3S,4R)-spiro[bicyclo[2.2.1]heptane-2,1'-cyclopropan]-3-ylmethyl]piperidine as clinical

期刊:Journal of medicinal chemistry发表年份:2009作者:Atsushi Satoh; Takeshi Sagara; Hiroki Sakoh; Masaya Hashimoto; Hiroshi Nakashima; Tetsuya Kato; Yasuhiro Goto; Sayaka Mizutani; Tomoko Azuma-Kanoh; Takeshi Tani; Shoki Okuda; Osamu Okamoto; Satoshi Ozaki; Yoshikazu Iwasawa; Hisashi Ohta; Hiroshi Kawa