Identification of MK-1925: a selective, orally active and brain-penetrable opioid receptor-like 1 (ORL1) antagonist.

Kensuke Kobayashi,Tomohiro Tsujita,Hirokatsu Ito,Satoshi Ozaki,Takeshi Tani,Yasuyuki Ishii,Shoki Okuda,Kiyoshi Tadano,Takahiro Fukuroda,Hisashi Ohta,Osamu Okamoto

Bioorganic & Medicinal Chemistry Letters（2009）

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摘要

We report identification of 3-[5-(3,5-difluorophenyl)-3-({[(1S,3R)-3-fluorocyclopentyl]amino}methyl)-4-methyl-1H-pyrazol-1-yl]propanenitrile 39 (MK-1925) as a selective, orally available and brain-penetrable opioid receptor-like 1 (ORL1) antagonist. 39 was orally active in the in vivo locomotor test as well as good brain penetrability in mice.

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关键词

ORL1 antagonist,Nociceptin/orphanin FQ,Arylpyrazole

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