Discovery and in vitro and in vivo profiles of 4-fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as novel class of an orally active metabotropic glutamate receptor 1 (mGluR1) antagonist |
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| Authors: | Atsushi Satoh Yasushi Nagatomi Yukari Hirata Satoru Ito Gentaroh Suzuki Toshifumi Kimura Shunsuke Maehara Hirohiko Hikichi Akio Satow Mikiko Hata Hisashi Ohta Hiroshi Kawamoto |
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| Institution: | aTsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan |
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| Abstract: | We identified 4-fluoro-N-4-6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide 27 as a potent mGluR1 antagonist. The compound possessed excellent subtype selectivity and good PK profile in rats. It also demonstrated relatively potent antipsychotic-like effects in several animal models. Suitable for development as a PET tracer, compound 27 would have great potential for elucidation of mGluR1 functions in human. |
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| Keywords: | mGluR1 antagonist Antipsychotic Biarylamide |
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