ML204 HYDROCHLORIDE
ML204 HYDROCHLORIDE 用途与合成方法
|
TRPC4
|
TRPC5
|
ML204 hydrochloride inhibits TRPC4β-mediated intracellular Ca
2+
rise with an IC
50
value of 0.96 μM (HEK293 cells) and exhibits 19-fold selectivity against muscarinic receptor-coupled TRPC6 channel activation.
ML204 hydrochloride blocks TRPC4β activity induced through either G
i/o
stimulation by μ-opioid, 5HT
1A
serotonin, and M
2
muscarinic receptors or G
q/11
stimulation by the endogenous M
3
-like muscarinic receptors.
ML204 hydrochloride blocks LPS-induced TRPC5 channel activity.
ML204 hydrochloride (1 mg/kg; s.c.; twice a day; for 5 days) causes mortality associated with exacerbated hypothermia and decreases peritoneal leukocyte numbers and cytokines in LPS-injected mice.
| Animal Model: | Nonfasted male C57BL/6 (2-3 months) |
| Dosage: | 1 mg/kg |
| Administration: | Subcutaneous injection, twice a day, for 5 days (prior to LPS injection) |
| Result: | Induces mortality associated with increased hypothermia in mice with LPS-induced systemic inflammatory response. |
