2070015-10-8

ML204 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.
It 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.
It blocks LPS-induced TRPC5 channel activity.

ML204 (1 mg/kg; sc; twice a day; for 5 days) causes mortality associated with exacerbated hypothermia and decreases peritoneal leukocyte numbers and cytokines in LPS-injected mice.