New μ-Opioid Receptor Agonists with Piperazine Moiety

Teruo KOMOTO; Tomomi OKADA; Susumu SATO; Yasuhiro NIINO; Tetsuo OKA; Takao SAKAMOTO

doi:10.1248/cpb.49.1314

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New μ-Opioid Receptor Agonists with Piperazine Moiety

Teruo KOMOTO, Tomomi OKADA, Susumu SATO, Yasuhiro NIINO, Tetsuo OKA, Takao SAKAMOTO

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Keywords: μ-opioid receptor agonist, piperazine, Pd-catalyzed amination, cross-coupling

JOURNAL FREE ACCESS

2001 Volume 49 Issue 10 Pages 1314-1320

DOI https://doi.org/10.1248/cpb.49.1314

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Abstract

New μ-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.

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