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New mu-opioid receptor agonists with piperazine moiety
1Central Research Labs., SSP Co., Ltd., Narita, Chiba, Japan. Teruo.Komoto@ssp.co.jp
Chemical & Pharmaceutical Bulletin
|October 19, 2001
Abstract:
New mu-opioid receptor (MOR) agonists containing piperazine and homopiperazine moieties in the structures were synthesized and their affinities to and agonist potencies on MOR were evaluated. Among the synthesized compounds, 4-[4-(2-methoxyphenyl)piperazin-1-yl]-N,N-dimethyl-2,2-diphenylbutanamide (20 Aa) showed the highest affinity to the human MOR expressed in Chinese hamster ovary (CHO)-K1 cells, and the highest agonist potency on the MOR in isolated guinea-pig ileum preparation.