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Identification and characterization of a selective radioligand for melanin-concentrating hormone 1-receptor (MCH1R) |
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| Authors: | Masahiko Ito Toshihiro Sakamoto Takao Suzuki Shinichiro Egashira Minoru Moriya Akane Ishihara Hisashi Iwaasa Hiroko Matsushita Kazuho Nakase Michael A Wallace Dennis Dean Nagaaki Sato Shigeru Tokita Akio Kanatani |
| Institution: | 1. Department of Metabolic Disorder, Tsukuba Research Institute, BANYU Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan;2. Department of Medicinal Chemistry, Tsukuba Research Institute, BANYU Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan;3. Department of Pharmacology, Tsukuba Research Institute, BANYU Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan;4. Merck Research Laboratories, Rahway, NJ 07065, USA |
| Abstract: | We have developed and characterized 35S]4a as a potent and selective radioligand for melanin-concentrating hormone 1-receptor (MCH1R). Compound 35S]4a showed appreciable specific signals in brain slices prepared from wild-type mice but not from MCH1R deficient mice, confirming the specificity and utility of 35S]4a as a selective MCH1R radioligand for ex vivo receptor occupancy assays. |
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