Chemical Structure : GW117
货号: PC-22026Not For Human Use, Lab Use Only.
GW117 is a novel serotonin (5-HT2C) receptor antagonist and melatonin (MT1 /MT2 ) receptor agonist with Ki values of 0.32, 0.12, and 54 nM, respectively.
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GW117 is a novel serotonin (5-HT2C) receptor antagonist and melatonin (MT1 /MT2 ) receptor agonist with Ki values of 0.32, 0.12, and 54 nM, respectively.
GW117 stimulates specific [35S]‐GTPγS binding with an EC50 of 2.49 nM and 1.54 nM and a maximal increase over basal binding (% Emax) of 104 ± 7.34% and 103.2 ± 4.56% on the MT1 receptor and MT2 receptor, respectively.
GW117 dose‐dependently blocked activation of [35S]‐GTPγS binding and [3H]PIP released by 10 nM 5‐HT.
GW117 (20, and 40 mg/kg, p.o.) markedly reduced the immobility time on TST test in mice, showed potential antidepressant‐like activity.
分子量 | 280.77 | |
分子式 | C15H13D3ClNO2 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Gao N, et al. CNS Neurosci Ther. 2021 Jun;27(6):702-713.
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