An antagonist of mGluR1
FITM is an antagonist of metabotropic glutamate receptor 1 (mGluR1; IC50 = 5.1 nM for the human receptor).1 It is selective for mGluR1 over mGluR2, mGluR5, and mGluR8 (IC50s = >10, 7, and >10 ?M, respectively). FITM (0.3 mg/kg) decreases methamphetamine-induced hyperlocomotion in mice and reverses disruptions in prepulse inhibition induced by methamphetamine and ketamine in rats when administered at a dose of 1 mg/kg.
1.Satoh, A., Nagatomi, Y., Hirata, Y., et al.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) antagonistBioorg. Med. Chem. Lett.19(18)5464-5468(2009)
Animal experiment: | Rats: Sprague–Dawley rats are treated with different doses of unlabeled FITM (0, 1, 5, or 30 μg/kg or 1 mg/kg) just before a bolus injection of 18F-FITM (17–18 MBq, 30–40 pmol, 0.1 mL). Estimations of equilibrium state and BPND were acquired[3]. |
参考文献: [1]. Wu H, et al. Structure of a class C GPCR metabotropic glutamate receptor 1 bound to an allosteric modulator. Science. 2014 Apr 4;344(6179):58-64. | |
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