生物活性 | |||
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描述 | Ro 5212773, also known as EPPTB, is a potent and selective TAAR1 antagonist (Ki=0.9 nM for mouse TAAR1) and has no significant effect on other TAARs[1][2].Ro 5212773 inhibits excitability of hippocampal pyramidal neurons and also reduces seizure-like events (SLE) and seizure activity[1].Ro 5212773 blocked TAAR1-mediated inwardly rectifying K+ current activation. Ro 5212773 effectively antagonised 1.5 μM β-phenylethylamine activation of cAMP production induced by TAAR1 in mice (IC50= 27.5 nM). The antagonistic effect of Ro 5212773 on cAMP production in mice was significantly stronger compared to TAAR1 in rat (IC50= 4539 nM) and human (IC50= 7487 nM)[2]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.64mL 0.53mL 0.26mL |
13.21mL 2.64mL 1.32mL |
26.43mL 5.29mL 2.64mL |