Potent, selective melanin-concentrating hormone receptor 1 (MCH1
R) antagonist (IC50
= 5.6 nM in hMCH1
R-expressing CHO cells). Displays selectivity for MCH1
R over MCH2
= > 10 μ
M). Decreases body weight in a mouse model of diet-induced obesity. Brain penetrant; orally active.
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All Tocris products are intended for laboratory research use only.
Discovery of novel phenylpyridone derivatives as potent and selective MCH1R antagonists.
Haga et al.
Melanin-concentrating hormone 1-receptor antagonist suppresses body weight gain correlated with high receptor occupancy levels in diet-induced obesity mice.
Ito et al.