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New m-Opioid Receptor Agonists .
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Chem. Pharm. Bull. 49(10) 1314—1320 (2001) Vol. 49, No. 10
New m-Opioid Receptor Agonists with Piperazine Moiety
Teruo KOMOTO,*,a,c Tomomi OKADA,a Susumu SATO,a Yasuhiro NIINO,b Tetsuo OKA,b and
New m-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 (20Aa) 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.