712313-35-4
712313-35-4 結(jié)構(gòu)式
物理化學(xué)性質(zhì)
常見問題列表
|
CysLT 2
|
In a CysLT
2
receptor reporter cell line, HAMI 3379 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. In contrast, HAMI 3379 exhibits very low potency on a recombinant CysLT
1
receptor cell line (IC
50
>10000 nM).
HAMI 3379 (ip; 0.025-0.4 mg/kg; 24 hours) attenuates the acute brain injury 24 hours after middle cerebral artery occlusion (MCAO) with effective doses of 0.1-0.4 mg/kg and a therapeutic window of ～1 hour. It attenuates the neurological deficits, and reduces infarct volume, brain edema, and neuronal loss and degeneration 24 and 72 hours after MCAO.
HAMI 3379 (infused into the aortic cannula at a rate of 1% of the total flow rate; 0.01, 0.1, 1 μM; 20 min) concentration-dependently inhibits and reverses the LTC
4
-induced perfusion pressure increase and contractility decrease.
| Animal Model: | Male Sprague-Dawley rats (250-300 g) after MCAO |
| Dosage: | 0.025, 0.05, 0.1, 0.2, 0.4 mg/kg |
| Administration: | IP; 24 hours |
| Result: | Attenuated the acute brain injury 24 hours after MCAO with effective doses of 0.1-0.4 mg/kg and a therapeutic window of ～1 hour. |