HAMI 3379

HAMI 3379 is a potent and selective CysLT 2 receptor antagonist. HAMI 3379 has a protective effect on acute and subacute ischemic brain injury, and attenuates microglia-related inflammation In Vitro In a CysLT 2 receptor reporter cell line, HAMI3379 antagonizes leukotriene D 4 - (LTD 4 -) and leukotriene C 4 - (LTC 4 -) induced intracellular calcium mobilization with IC 50 values of 3.8 nM and 4.4 nM respectively. HAMI3379 exhibits very low potency on a recombinant CysLT 1 receptor cell line (IC 50 >10000 nM). HAMI3379 does not exhibit any agonistic activity on both CysLT receptor cell lines. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo HAMI 3379 (0.025-0.4 mg/kg; ip) with 0.1-0.4 mg/kg significantly reduces the infarct volume and percentage increase in the ischemic/contralateral hemispheric ratio. HAMI3379 (0.1 mg/kg; ip) administered at 0 and 1 h after reperfusion reduces infarct volume, attenuated brain edema, reduced neurological score, and increased holdingangle. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Sprague-Dawley rats (250-300 g) after MCAODosage: 0.025, 0.05, 0.1, 0.2, 0.4 mg/kg Administration: IP Result: Significantly reduced the infarct volume and percentage increase inthe ischemic/contralateral hemispheric ratio (an index ofbrain edema) with 0.1-0.4 mg/kg. Significantly reduced the neurological deficit score. Form:Solid IC50& Target:CysLT 2

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