Ito Masahiko, Sakamoto Toshihiro, Suzuki Takao, Egashira Shinichiro, Moriya Minoru, Ishihara Akane, Iwaasa Hisashi, Matsushita Hiroko, Nakase Kazuho, Wallace Michael A, Dean Dennis, Sato Nagaaki, Tokita Shigeru, Kanatani Akio
Department of Metabolic Disorder, Tsukuba Research Institute, BANYU Pharmaceutical Co., Ltd, Okubo, Ibaraki, Japan.
Bioorg Med Chem Lett. 2009 May 15;19(10):2835-9. doi: 10.1016/j.bmcl.2009.03.102. Epub 2009 Mar 26.
We have developed and characterized [(35)S]4a as a potent and selective radioligand for melanin-concentrating hormone 1-receptor (MCH1R). Compound [(35)S]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 [(35)S]4a as a selective MCH1R radioligand for ex vivo receptor occupancy assays.
我们已经研发并鉴定了[(35)S]4a，它是一种用于黑色素浓缩激素1受体（MCH1R）的强效且选择性的放射性配体。化合物[(35)S]4a在野生型小鼠制备的脑切片中显示出明显的特异性信号，但在MCH1R缺陷型小鼠的脑切片中未显示，这证实了[(35)S]4a作为用于体外受体占有率测定的选择性MCH1R放射性配体的特异性和实用性。
