1181081-71-9
1181081-71-9 結(jié)構(gòu)式
基本信息
化合物 T14984
(5Z)-5-[(4-Fluoro-2-hydroxyphenyl)methylene]-2-(tetrahydro-1-(2H)-pyridazinyl)-4(5H)-thiazolone
4(5H)-Thiazolone, 5-[(4-fluoro-2-hydroxyphenyl)methylene]-2-(tetrahydro-1(2H)-pyridazinyl)-, (5Z)-
物理化學(xué)性質(zhì)
常見(jiàn)問(wèn)題列表
EC50: 616 nM (KCC2)
There is no change in [Cl ? ] i in HEK293-cl cells when incubated with CLP257, indicating inactivity on NKCC1, KCC1, KCC3 or KCC4. Oocyte pre-incubation with CLP257 (200 nM) increases KCC2 transport activity by 61%, but causes no change in other CCCs. Functional, dose-dependent antagonism is also observed between CLP257 and the recently characterized KCC2 antagonist VU024055119. CLP257 (50 μM) provokes < 0.2% of the effect of 5 μM muscimol in CHO cells transduced with recombinant α1β2γ2 GABAA receptors, indicating negligible agonist activity of CLP257 on GABAA receptors.
CLP257 (100?mg/kg; intraperitoneal injection; adult male rats) treatment induced a significant increase in mechanical sensitivity.
| Animal Model: | Adult male rats (300?g) injected with Morphine |
| Dosage: | 100?mg/kg |
| Administration: | Intraperitoneal injection |
| Result: | Induced a significant increase in mechanical sensitivity. |