生物活性 | |||
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描述 | Transient receptor potential canonical (TRPC) channels are Ca2+-permeable nonselective cation channels implicated in diverse physiological functions, including smooth muscle contractility and synaptic transmission[3]. ML204 is a novel, potent, and selective TRPC4 channel inhibitor with apparent IC50 values of about 1 μM in fluorescent intracellular Ca2+ assays and about 3 μM in whole-cell voltage clamp experiments[3]. ML204 blocked TRPC4β activity induced through either Gi/o stimulation by μ-opioid, 5HT1A serotonin, and M2 muscarinic receptors or Gq/11 stimulation by the endogenous M3-like muscarinic receptors. It also blocked TRPC4β channels activated by intracellularly applied GTPγS (guanosine 5'-3-O-(thio) triphosphate) or Ca2+, which bypass receptor stimulation[3]. In isolated guinea pig ileal myocytes, ML204 blocked muscarinic cation currents activated by bath application of carbachol or intracellular infusion of GTPγS, demonstrating its effectiveness on native TRPC4 currents[3]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
4.42mL 0.88mL 0.44mL |
22.09mL 4.42mL 2.21mL |
44.19mL 8.84mL 4.42mL |
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